S1573 |
Fasudil HCl
|
Fasudil HCl是一种有效的、具有选择性的Rho抑制剂(ROCK2, Ki=0.33 μM),同时对PKA、PKG、PKC和MLCK也具有抑制活性,Ki值分别为1.6 μM、1.6 μM、3.3 μM、36 μM。Fasudil 也是calcium channel的阻滞剂。 |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Sci China Life Sci, 2024, 67(8):1549-1562
-
CNS Neurosci Ther, 2024, 30(11):e70098
|
|
S1811 |
Amiloride HCl
|
Amiloride HCl是一种选择性的T-type calcium channel阻滞剂,epithelial sodium channel(ENaC)阻滞剂,urokinase plasminogen activator (uPA)抑制剂,Ki=7 μM。 |
-
J Extracell Vesicles, 2024, 13(4):e12426
-
J Extracell Vesicles, 2024, 13(4):e12426
-
Virus Res, 2024, 339:199258
|
|
S4202 |
Verapamil HCl
|
Verapamil HCl是L-型钙通道抑制剂,是第四类抗心律失常的药剂。Verapamil 可抑制 permeability-glycoprotein (P-gp) 和 CYP3A4。 |
-
J Immunother Cancer, 2024, 12(11)e009805
-
NPJ Precis Oncol, 2024, 8(1):94
-
Int J Mol Sci, 2024, 25(18)10162
|
|
S1808 |
Nifedipine
|
Nifedipine是一种二氢吡啶类钙离子通道阻滞剂,是有效的血管扩张剂,具有钙拮抗作用。 |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Laryngoscope Investig Otolaryngol, 2023, 8(5):1390-1400
-
Oncogene, 2021, 40(6):1128-1146
|
|
S2721 |
Nilvadipine
|
Nilvadipine (ARC029, FR34235,FK235) 是一种强效钙通道阻滞剂,IC50为0.03 nM。 |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Nat Commun, 2022, 13-1:6117
-
J Pers Med, 2022, 12(2)258
|
|
S2030 |
Flunarizine 2HCl
|
Flunarizine 2HCl (KW-3149, R14950) 是一种二氢盐酸盐,抑制钙离子通道,Ki为68 nM。 |
-
Sci Adv, 2023, 9(15):eadf2695
-
J Pers Med, 2022, 12(2)258
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
|
|
S1905 |
Amlodipine
|
Amlodipine (UK-48340) 是一种长效的钙离子通道抑制剂,用于降低血压缓解胸部疼痛。 |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Cancer Med, 2024, 13(11):e7291
-
Acta Pharm Sin B, 2023, 13(10):4217-4233
|
|
S6657 |
2-APB (2-Aminoethyl Diphenylborinate)
|
2-APB (2-Aminoethyl Diphenylborinate)是IP3 receptor的抑制剂,可以调节IP3诱导的钙释放。2-APB还可以抑制SOC通道的活性,并且在高浓度的时候可以激活TRP通道。 |
-
iScience, 2024, 27(8):110507
-
Mol Med Rep, 2024, 30(6)220
-
PLoS Pathog, 2023, 19(3):e1011295
|
|
S1293 |
Cilnidipine
|
Cilnidipine是一种L型和N型钙离子通道抑制剂,用来治疗高血压。 |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Nat Commun, 2021, 12(1):3907
-
Cell Discov, 2020, 6(1):96
|
|
S1748 |
Nisoldipine
|
Nisoldipine (Sular, BAY K 5552)是特定L型CaV1.2钙通道阻断剂,IC50为10 nM。 |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Biomed Pharmacother, 2022, 145:112432
-
iScience, 2022, 25(10):105068
|
|
S1356 |
Levetiracetam (UCB-L059)
|
Levetiracetam (UCB-L059, SIB-S1) 是一种抗癫痫化合物。Levetiracetam (UCB-L059, SIB-S1) 是 muscarinic acetylcholine receptors (mAChR) 的激动剂并能调节突触前P/Q型压敏钙离子通道 calcium (Ca2+) channel。 |
-
Front Neurosci, 2023, 17:1336026
-
bioRxiv, 2023, 2023.11.10.566574
-
Alzheimers Dement (N Y), 2022, 8(1):e12329
|
|
S8380 |
YM-58483 (BTP2)
|
YM-58483/BTP2是钙池调控钙离子进入(SOCE)的阻滞剂,参与调解不可兴奋细胞如淋巴细胞的激活。 |
-
Cell Death Discov, 2023, 9(1):100
-
Dev Cell, 2022, S1534-5807(21)01035-2
-
J Innate Immun, 2022, 1-13
|
|
S7924 |
Bay K 8644
|
Bay K 8644是一种高选择性的L型钙离子通道激动剂,EC50为17.3 nM。 |
-
ACS Nano, 2021, 10.1021/acsnano.1c03517
-
Cell Biol Toxicol, 2021, 10.1007/s10565-021-09615-y
-
Journal of Advanced Research, 2020, 10.1016/j.jare.2020.10.005
|
|
S3809 |
Imperatorin
|
Imperatorin (Ammidin, Marmelosin, Pentosalen, 8-Isoamylenoxypsoralen), a naturally occurring psoralen-type furanocoumarin, is a potent myorelaxant agent and acts as a calcium antagonist on vascular smooth muscle. |
-
Pharmaceuticals (Basel), 2023, 10.3390/ph16111595
-
Metabolites, 2022, 13(1)3
-
Adv Sci (Weinh), 2020, 7(16):2000925
|
|
S1662 |
Isradipine
|
Isradipine (PN 200-110)是一种高效选择性的L型压力控式钙离子通道抑制剂,用于治疗高血压。 |
-
J Cell Sci, 2022, 135(14)jcs260249
-
Environ Toxicol Chem, 2021, 10.1002/etc.5018
-
Cell Discov, 2020, 6(1):96
|
|
S2114 |
Dronedarone HCl
|
Dronedarone HCl (SR33589) 用于治疗阵发性和持续性房颤或房扑的患者。 |
-
Cancers (Basel), 2022, 14(19)4883
-
Chem Res Toxicol, 2021, 10.1021/acs.chemrestox.1c00127
-
Cell Syst, 2019, 8(2):97-108
|
|
S5478 |
Dantrolene sodium
|
Dantrolene sodium(F 440) acts as a postsynaptic muscle relaxant by inhibiting Ca2+ ions release from sarcoplasmic reticulum stores by antagonizing ryanodine receptors. |
-
Emerg Microbes Infect, 2024, 13(1):2399945
-
PLoS Pathog, 2023, 19(3):e1011295
-
Transl Stroke Res, 2022, 10.1007/s12975-022-01021-8
|
|
S1813 |
Amlodipine Besylate
|
Amlodipine Besylate是一种长效的钙离子通道抑制剂,IC50为1.9 nM。 |
-
Front Pharmacol, 2022, 13:902305
-
Cell Discov, 2020, 6(1):96
-
Oncogene, 2019, 38(1):120-139
|
|
S1425 |
Ranolazine 2HCl
|
Ranolazine 2HCl (RS-43285,RS 43285-193,Ranexa, renolazine,Ranolazine dihydrochloride)是一种钙离子通过 sodium/calcium channal摄取的抑制剂抗心绞痛药物,用于治疗慢性心绞痛。 |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Basic Clin Pharmacol Toxicol, 2023, 133(2):194-201
-
Cell Rep, 2022, 41(1):111445
|
|
S2482 |
Manidipine 2HCl
|
Manidipine 2HCl (CV-4093) 是Manidipine的盐酸盐形式,是钙通道阻断剂,IC50为2.6 nM,临床上常用于抗高血压。Phase 4。 |
-
Adv Sci (Weinh), 2023, 10(11):e2205500
-
Front Microbiol, 2023, 14:1177391
-
Environ Toxicol Chem, 2021, 10.1002/etc.5018
|
|
S1885 |
Felodipine
|
Felodipine (CGH-869) 是一种选择性L型Ca2+通道阻断剂,IC50为0.15 nM。 |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Bioact Mater, 2022, 14:272-289
-
Cell Discov, 2020, 6(1):96
|
|
S1747 |
Nimodipine
|
Nimodipine (BAY E 9736) 是一种二氢吡啶衍生物,是钙离子通道抑制剂Nifedipine的类似物,具有降压活性。Nimodipine能减少细胞内游离Ca2+,Beclin-1及细胞自噬。 |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Eye Vis (Lond), 2024, 11(1):37
-
Cell Discov, 2020, 6(1):96
|
|
S2017 |
Benidipine HCl
|
Benidipine HCl (KW-3049,(±)- Benidipine) 是Benidipine的盐酸盐形式,是一种二氢吡啶类的钙离子通道抑制剂。 |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Cell Discov, 2020, 6(1):96
-
ACS Infect Dis, 2020, acsinfecdis.0c00486
|
|
S3931 |
Ginsenoside Rd
|
Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively. |
-
Drug Des Devel Ther, 2022, 16:2767-2782
-
J Ginseng Res, 2022, 46(5):700-709
-
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
|
|
S2415 |
Astragaloside A
|
Astragaloside A是从黄芪中分离的一种纯化的皂苷,广泛应用于治疗心血管疾病。 |
-
Sci Rep, 2022, 12(1):7
-
Carcinogenesis, 2020, 41(7):993-1004
-
J Med Virol, 2019, 91(8):1440-1447
|
|
S1799 |
Ranolazine
|
Ranolazine (CVT 303, RS 43285-003)是一种钙离子通过 sodium/calcium channal摄取的抑制剂抗心绞痛药物,用于治疗慢性心绞痛。 |
-
Sci Rep, 2023, 10.1038/s41598-023-47540-8
-
Cancer Cell, 2022, S1535-6108(22)00312-9
|
|
S2535 |
Econazole nitrate
|
Econazole Nitrate (NSC 243115,Spectazole) 是一种咪唑类抗真菌药物。 |
-
Nat Commun, 2024, 15(1):8708
-
Cell Rep Med, 2023, 4(12):101309
-
Int J Mol Sci, 2022, 23(22)13809
|
|
S4181 |
Nicardipine HCl
|
Nicardipine HCl (RS-69216,YC-93)是二氢吡啶的钙通道抑制剂,具有显著的血管扩张作用。 |
-
Cell Discov, 2020, 6(1):96
-
ACS Infect Dis, 2020, acsinfecdis.0c00486
|
|
S3053 |
Azelnidipine
|
Azelnidipine (UR-12592)是一种二氢吡啶类钙通道阻断剂。 |
-
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X
-
Environ Toxicol Chem, 2021, 10.1002/etc.5018
|
|
S1865 |
Diltiazem HCl
|
Diltiazem (Tiazac, RG 83606) HCl 是一种Benzothiazepine衍生物,具有舒张血管的作用,由于其抑制钙离子在膜的功能。 |
-
J Immunother Cancer, 2024, 12(11)e009805
-
J Cell Mol Med, 2018, 22(12):5964-5977
-
FASEB J, 2017, 31(2):625-635
|
|
S2397 |
Palmatine chloride
|
Palmatine chloride 是Palmatine的盐酸盐,是一种小檗碱类生物碱。 |
-
Molecules, 2021, 26(5)1210
-
J Med Virol, 2019, 91(8):1440-1447
|
|
S4648 |
Dantrolene sodium hemiheptahydrate
|
Dantrolene sodium hemiheptahydrate (Dantrium) 是一种骨骼肌松弛药,通过干扰肌纤维中的兴奋-收缩偶联起作用。 |
-
Cardiovasc Res, 2021, 117(4):1091-1102
-
Oxid Med Cell Longev, 2021, 2021:8810698
|
|
S6847 |
ML-9 HCl
|
ML-9 HCl (ML-9 hydrochloride) 是一种有效的选择性的 Akt kinase、myosin light chain kinase (MLCK) 和 stromal interaction molecule 1 (STIM1)。ML-9 HCl 也是 Ca2+-permeable channels 的有效抑制剂。ML-9 HCl 是一种靶向自噬和细胞死亡的亲溶酶体剂。 |
-
PLoS Pathog, 2023, 19(3):e1011295
-
J Mol Endocrinol, 2019, 63(3):199-213
|
|
S2481 |
Manidipine
|
Manidipine(CV-4093,(±)-Manidipine)是一种二氢吡啶类钙拮抗剂,用于治疗高血压。 |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Antiviral Res, 2018, 150:130-136
|
|
S2446 |
Levosimendan
|
Levosimendan(OR1259,OR1855,Simsndan) 是一种钙增敏剂,通过与cardiac troponin C (cTnC)结合而发挥作用,这种作用具有钙依赖性。 |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Antiviral Res, 2017, 146:76-85
|
|
S2080 |
Clevidipine Butyrate
|
Clevidipine Butyrate(Cleviprex)是一种二氢吡啶类钙离子通道抑制剂,用于降血压。 |
-
J Immunother Cancer, 2024, 12(11)e009805
-
ACS Infect Dis, 2020, acsinfecdis.0c00486
|
|
S2573 |
Tetracaine HCl
|
Tetracaine HCl (Amethocaine hydrochloride)是Tetracaine的盐酸盐形式,是一种有效的局部麻醉剂和通道功能变构酶抑制剂。 |
-
PLoS Pathog, 2023, 19(3):e1011295
|
|
S5255 |
Nicardipine
|
Nicardipine is a potent calcium channel blockader with marked vasodilator action. |
-
Cell Chem Biol, 2021, S2451-9456(21)00442-6
|
|
S4626 |
Ethosuximide
|
Ethosuximide(Zarontin)是一种琥珀酰亚胺类的抗痉挛试剂,主要用于失神发作。是钙离子通道阻滞剂。 |
-
Nature, 2018, 554(7692):317-322
|
|
S5966 |
Amlodipine maleate
|
Amlodipine (Amvaz, UK-48340) maleate 是一种长效的 calcium channel 的阻滞剂,可用于降低血压或预防胸痛。 |
-
Front Pharmacol, 2022, 13:902305
|
|
S4597 |
Lercanidipine hydrochloride
|
Lercanidipine是二氢吡啶类的钙离子通道抑制剂。 |
-
J Immunother Cancer, 2024, 12(11)e009805
-
J Phys Chem B, 2013, 117(23):6868-73
|
|
S4977 |
Efonidipine
|
Efonidipine (NZ-105) 是一种L型和T型钙离子通道阻滞剂,可引起血管舒张和心脏自律性降低。它还能抑制醛固酮从肾上腺分泌。 |
-
Biomol Ther (Seoul), 2022, 30(5):455-464
|
|
S5191 |
Cinacalcet
|
Cinacalcet (AMG073, Sensipar, Cin) 是一种口服活性的 receptors for calcium (CaR) 的变构激动剂,可增加CaR对Ca的敏感性。 |
-
Int J Mol Sci, 2022, 23(8)4323
|
|
S6834 |
Zegocractin (CM 4620)
|
Zegocractin (CM 4620)是一种 calcium-release activated calcium-channel (CRAC channel) 的抑制剂。CM4620 抑制Orai1/STIM1介导的Ca2+电流和Orai2/STIM1介导的电流,对应的IC50值分别接近120 nM和900 nM。 |
-
Elife, 2023, 12e81288
|
|
S5514 |
Lanthanum(III) chloride heptahydrate
|
Lanthanum(III) chloride is the inorganic compound used in biochemical research to block the activity of divalent cation channels, mainly calcium channels. |
-
J Surg Res, 2021, 263:236-244
|
|
S3766 |
Tanshinone IIA sulfonate sodium
|
Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA isolated as the main pharmacologically active natural compound from a traditional Chinese herbal medicine, the dried root of Salvia miltiorrhiza Bunge known as Danshen. Sodium tanshinone IIA sulfonate (STS) is a potent negative allosteric modulator of the human purinergic receptor P2X7. Sodium tanshinone IIA sulfonate (STS) inhibits the activity of CYP3A4 and store-operated Ca2+ entry (SOCE) through store-operated Ca2+ channels (SOCC) via downregulating the expression of transient receptor potential canonical proteins (TRPC). |
-
J Inflamm Res, 2022, 15:6293-6306
|
|
S3674 |
Levamlodipine
|
Levamlodipine (S-amlodipine) is a pharmacologically active enantiomer of amlodipine which belongs to the dihydropyridine group of calcium channel blocker. It acts on the L-type of calcium channels and its treatment results in vasodilation and a fall in blood pressure. |
-
Oncogene, 2021, 40(6):1128-1146
|
|
S7074 |
Ionomycin
|
Ionomycin (SQ23377) 是一种有效的选择性钙离子载体,也是由Streptomyces conglobatus产生的抗生素。 它诱导蛋白激酶C (PKC)的激活并促进细胞凋亡。 |
-
Diabetes, 2024, db231000
-
Am J Physiol Cell Physiol, 2020, 10.1152/ajpcell.00290.2020
|
|
S4727 |
Cinnarizine
|
Cinnarizine (Stugeron, Dimitronal, Stutgin, Cinarizine)是piperazine的药物衍生物,是抗组胺剂和钙离子通道阻滞剂。 |
-
Sci Adv, 2022, 8(15):eabk2376
|
|
S1994 |
Lacidipine
|
Lacidipine (GX-1048, GR-43659X, SN-305)是一种L-型钙离子通道抑制剂。 |
-
J Immunother Cancer, 2024, 12(11)e009805
|
|
S2491 |
Nitrendipine
|
Nitrendipine (Bayotensin) 是一种二氢吡啶类钙离子通道抑制剂,IC50为95 nM。 |
-
Nat Commun, 2024, 15(1):8708
|
|
S2050 |
Strontium Ranelate
|
Strontium Ranelate 是Ranelic acid的锶(II)盐,用于(-)-Desmethoxyverapamil结合到钙离子通道,IC50为0.5 mM。 |
|
|
S1911 |
Disodium Cromoglycate
|
Disodium Cromoglycate (Gynazole ,FPL 670 (Cromolyn) Disodium,Cromolyn sodium) 是一种抗过敏药,IC50为39 μg/mL。 |
|
|
S0000 |
Cav 2.2 blocker 1
|
Cav 2.2 blocker 1 (compound 9) 是一种 N-type calcium channel (Cav 2.2) 阻滞剂可用于治疗疼痛,其IC50值为0.001 μM。 |
|
|
S0713 |
S107 hydrochloride
|
S107 hydrochloride 是一种 RyR2 (type 2 ryanodine receptor)/FKBP12.6 (FK506 binding protein 12.6) complex 的特异性稳定剂,会影响 Ca2+ 信号传导。 |
|
|
E0778 |
o-3M3FBS
|
O-3M3FBS是m-3M3FBS的阴性对照,以独立于PLC的机制及拮抗的方式抑制内向和外向电流,可逆地抑制延迟整流K+通道,以与m-3M3FBS竞争的形式增加[Ca2+](i)。 |
|
|
S3236 |
Mesaconitine
|
Mesaconitine 是Aconiti tuber附子块茎中的附子生物碱之一,通过从细胞外空间流入Ca2+来增加内皮细胞中的[Ca2+]i水平。 |
|
|
S6994 |
TD-165
|
TD-165 是基于 PROTAC 技术的 CRBN 降解剂。 TD-165 包括一个 CRBN 配体结合基团,一个 linker 和一个 VHL 结合基团。 |
|
|
E4039 |
(S)-(-)-Bay K8644
|
(S)-(-)-Bay K8644是Bay K 8644的传统外消旋混合物,是电压敏感的L型钙通道激动剂。 它还可激活 Ba2+ 电流 (Iba),EC50 为 32 nM。 |
|
|
S4931 |
Propiverine hydrochloride
|
Propiverine是一种抗胆碱能药物,用于治疗膀胱过度活动症和尿失禁。 |
|
|
E1259 |
DNQX
|
DNQX是一种AMPA受体拮抗剂,可通过电压门控钙通道防止过多的钙流入。 |
|
|
S3045 |
Cinepazide maleate
|
Cinepazide maleate是cinepazide的马来酸盐形式,而cinepazide是一种血管舒张药。 |
-
J Immunother Cancer, 2024, 12(11)e009805
|
|
S3242 |
Loureirin B
|
Loureirin B (LB, LrB),是从Dracaena cochinchinensis中提取的类黄酮,是 PAI-1 的抑制剂,其IC50值为26.10 μM。Loureirin B 可下调TGF-β1刺激的成纤维细胞中的 p-ERK 和 p-JNK。Loureirin B 主要通过增加Pdx-1、MafA、细胞内ATP水平来促进胰岛素分泌,抑制 KATP 电流,Ca2+ 进入细胞内。 |
|
|
E1879New |
CBD3063
|
CBD3063(EX-A8428) 是一种选择性、同类首创的 Cav2.2-CRMP2(ollapsin 反应介质蛋白 2)相互作用抑制剂。它可抑制 Cav2.2 和 N 型(Cav2.2)钙电流的表面运输。CBD3063 变构调节 Cav2.2 以实现镇痛和缓解疼痛,且无不良副作用。 |
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S0535 |
FK962
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FK962是FK960的衍生物,具有抗痴呆的特性,在1-1000 nM时,显著增强高K+诱导的大鼠海马片的生长抑素释放,在1-100 nM时,也显著降低生长抑素诱导的大鼠海马神经元的Ca2+通道抑制。 |
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S0870 |
Barnidipine
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Barnidipine (Libradin, Mepirodipine, Vasexten, YM-09730-5, Cyress, Hypoca, Oldeca) 是一种降压药,属于dihydropyridine (DHP)组的calcium 拮抗剂 (CaA),对[3H]nitrendipine 结合位点的Ki值为0.21 nM。 |
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S0973 |
Wilforgine
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Wilforgine 是 Tripterygium wilfordii Hook. F.中主要的生物活性倍半萜生物碱之一,可在M. separata larvae的肌肉中诱导显微结构和超微结构变化,其发挥作用的位置是肌肉系统中的 calcium receptors or channels。 |
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E4919New |
Barnidipine hydrochloride
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Barnidipine hydrochloride(Mepirodipine hydrochloride, YM-09730-5) 是一种L 型钙 (CaA) 拮抗剂。它对 [3H]initrendipine结合位点具有高亲和力,Ki 值为 0.21 nmol/l。Barnidipine hydrochloride也可用作抗高血压药。 |
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S5279 |
Fendiline hydrochloride
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Fendiline hydrochloride is the hydrochloride salt form of Fendiline, which is an L-type calcium channel blocker and also a specific inhibitor of K-Ras plasma membrane targeting with no detectable effect on the localization of H- and N-Ras. |
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S3845 |
Panaxadiol
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Panaxadiol (20(R)-Panaxadiol) is a triterpene sapogenin originally found in species of Panax (ginseng) and exhibits anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities. It inhibits Ca2+ channels, decreasing channel open time and open state probability in vitro and displaying anti-arrhythmic potential. |
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S5898 |
Efonidipine hydrochloride monoethanolate
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Efonidipine (NZ-105) hydrochloride monoethanolate 是一种L型和T型 calcium channel 的阻滞剂,可导致血管舒张并降低心脏的自动节律性。Efonidipine hydrochloride monoethanolate 还抑制肾上腺醛固酮的分泌。 |
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E4980New |
Verapamil
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Verapamil(Iproveratril,Dilacoran) 是一种苯烷基胺衍生物,是钙内流的拮抗剂,也是P-gp和CYP3A4的抑制剂。它对治疗心绞痛、心律失常、心肌病和高血压有疗效。 |
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Cell Death Dis, 2024, 15(11):855
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S3700 |
DHBP dibromide
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DHBP (1,1'-diheptyl-4,4'-bipyridinium),一种用于电致色记忆显示剂的紫罗碱,抑制由2 mM咖啡因和2 μg/ml多熔素诱导的钙释放,IC50分别为5 μg/ml和4 μg/ml。 |
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E1368 |
PD173212
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PD173212(Compound 11) 是一种选择性N 型电压敏感钙通道 (N-type voltage sensitive calcium channel, VSCC) 阻滞剂,在 IMR-32 测定中的 IC50 为 36 nM。 |
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E0936 |
IGS-1.76
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IGS-1.76是一种蛋白-蛋白相互作用(protein-protein interaction, PPI)抑制剂,具有药物样特性,对人类神经钙传感蛋白1(human neuronal calcium sensor 1, hNCS-1)具有显著的亲和力,并有效地调节hNCS-1和鸟嘌呤交换因子Ric8a的相互作用。 |
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S9017 |
Columbianadin
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Columbianadin (Zosimin, 2-Butenoic acid) 是一种来自当归的天然香豆素,已知具有多种生物活性,包括钙通道阻断活性、对各种癌细胞系的细胞毒活性、镇痛活性、肠道吸收和运输、抗炎和抗癌作用。 |
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S2403 |
Tetrandrine
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Tetrandrine是来源于千金藤根部的一种双苯基异喹啉,一种钙离子通道抑制剂。 |
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Pharmacol Res, 2024, 207:107314
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mBio, 2024, e0228723.
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Int J Mol Sci, 2024, 25(22)12330
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S9315 |
Praeruptorin A
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Praeruptorin A, a naturally existing pyranocumarin, is isolated from the dried root of Peucedanum praeruptorum Dunn. Praeruptorin A inhibits p38/Akt-c-Fos-NFATc1 signaling and PLCγ-independent Ca2+ oscillation. Praeruptorin A can significantly upregulates multidrug resistance-associated protein 2 expression via the constitutive androstane receptor-mediated pathway in vitro, and this should be taken as an herb-drug interaction. |
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E3642 |
Haliotidis concha Extract
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Haliotis Concha Extract从石决明Haliotis Concha的壳中提取,影响钙通道、PMCA1 mRNA的表达,并调节离子钙通道和钙-ATP酶。 |
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S6920 |
SEA0400
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SEA0400 是一种选择性的 Na+-Ca2+ exchanger (NCX) 的强效抑制剂,可抑制神经细胞、星形胶质细胞和小胶质细胞中Na+依赖性的Ca2+吸收,对应的IC50值分别为33 nM、5.0 nM和8.3 nM。SEA0400 可防止硝普钠 (SNP) 提高 ERK 和 p38 MAPK 的磷酸化和通过细胞外Ca2+依赖的方式增强reactive oxygen species (ROS) 的产生。 |
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F0840New |
IP3 Receptor 1 Rabbit mAb
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IP3 receptor,IP3 Receptor 1 |
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S4084 |
Lomerizine 2HCl
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Lomerizine dihydrochloride (KB-2796) 是一种相对较新的L-和T-型钙通道阻滞剂,用于治疗偏头痛。 |
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Nat Commun, 2024, 15(1):8708
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E0826 |
Levamlodipine Besylate
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Levamlodipine Besylate是一种强大的二氢吡啶钙通道(dihydropyridine calcium channel)阻滞剂,具有血管舒张特性,用于高血压和心绞痛的治疗。 |
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E0945 |
BIA
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BIA (TMBIM6 antagonist BIA)是一个潜在的TMBIM6拮抗剂,可以阻断TMBIM6和mTORC2的相互作用,最终阻断AKT的激活和癌症进展。 |
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S3682 |
Ethyl 3-Aminobenzoate methanesulfonate
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Ethyl 3-Aminobenzoate (Ethyl m-Aminobenzoate, NSC 93790, Tricaine) 可通过voltage-dependent Na+-channels阻止动作电位的产生,常用于鱼类的麻醉、镇静和安乐死。 |
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E0334 |
BAMB-4
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BAMB-4 (ITPKA-IN-C14)是一种新型的膜透性的肌醇三磷酸3-激酶A(Inositol-Trisphosphate 3-Kinase A, ITPKA)抑制剂,在ADP-Glo激酶检测中,IC50为37 μM。 |
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S9400 |
Rhynchophylline
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Rhynchophylline (Mitrinermine), an active component isolated from species of the genus Uncaria, acts as a calcium channel blocker and is widely used in traditional Chinese medicine mainly for treating ailments of central nervous and cardiovascular systems, such as lightheadedness, convulsions, numbness, and hypertension. |
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E0777 |
Z944
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Z944是一种高度选择性的T型钙通道拮抗剂,对hCaV3.1、hCaV3.2和hCaV3.3的IC50分别为50、160、110 nM。 |
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S3883 |
Protopine
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Protopine (Corydinine, Fumarine, Biflorine, Macleyine), an alkaloid present in different plants, has been shown to exhibit a number of activities, such as inhibition of calcium influx through both voltage and receptor-operated channels and inhibition of rabbit blood platelet aggregation. It also possesses anti-cholinergic and anti-histaminic as well as anti-bacterial activities. |
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S3191 |
Azumolene
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Azumolene(EU4093 free base)是一种等效的丹曲林(dantrolene)类似物,是一种兰尼碱受体 (ryanodine receptor, RyR) 调节剂,可抑制钙释放。 |
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S5567 |
Trimethadione
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Trimethadione is an oxazolidinedione anticonvulsant and often used to treat epileptic conditions that are resistant to other treatments. |
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S4353 |
Terfenadine
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Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9. |
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S9566 |
Bepridil hydrochloride
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Bepridil hydrochloride(CERM 1978)是一种抗心绞痛的药物,是钙离子通道(calcium channel)阻滞剂。它能阻止多种其他离子通道,包括钠离子和钾离子通道。 |
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S2436 |
Pranidipine
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Pranidipine (Acalas, OPC 13340)是一种新型的1,4-二氢吡啶 calcium channel 阻滞剂。Pranidipine可以增强cyclic GMP依赖性一氧化氮诱导的大鼠主动脉舒张。 |
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S0452 |
NP118809
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NP118809(39-1B4)是一种有效的N型钙通道(N-type calcium channel)阻滞剂,IC50为0.11 μM,对L型钙通道(L-type calcium channel)的抑制作用也较弱,IC50为12.2 μM。 |
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S2975 |
CarboxyaMidotriazole orotate
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Carboxyamidotriazole Orotate (L-651582 Orotate)是Carboxyamidotriazole (CAI)的乳清酸盐形式,它是一种口服生物可利用的信号转导抑制剂。Carboxyamidotriazole Orotate是一种非电压操作的钙通道和钙通道介导的信号通路的细胞抑制抑制剂。 Carboxyamidotriazole Orotate能够抑制肿瘤生长、侵袭、转移和血管生成。 |
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E2691 |
BAPTA tetrapotassium salt
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BAPTA tetrapotassium salt (BAPTA tetrapotassium)是一种不可渗透的、选择性的细胞外钙螯合剂,对Ca2+的亲和力比Mg2+高105倍,是研究钙在细胞信号转导中的作用的重要工具。 |
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S0016 |
SN-6
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SN-6 是一种选择性的 Na+/Ca2+ exchanger (NCX) 抑制剂。SN-6 可抑制NCX1、NCX2和NCX3,对应的IC50值分别为2.9 μM、16 μM和8.6 μM。SN-6 可消除 acetylcholine (ACh) 诱导的血管舒张。 |
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S9151 |
Praeruptorin E
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Praeruptorin E, isolated from Peucedanum praeruptorum Dunn., is a cardiotonic agent with selective cardiac calcium channel agonistic effect. |
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S6473 |
Pinaverium bromide
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Pinaverium bromide (Icosapentaenoic acid)是calcium channel阻滞剂,适用于治疗功能性胃肠病。 |
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Cell Rep, 2024, 43(11):114952
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E1410 |
Fluspirilene
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Fluspirilene(R 6218; Redeptin) 是一种L 型钙通道的非竞争性拮抗剂,在无细胞测定中 IC50 为 0.03 μM。 Fluspirilene 是一种注射长效抗精神病药,用于治疗精神分裂症。 |
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E2984 |
GSK-7975A
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GSK-7975A 是一种有效的口服 CRAC 通道抑制剂。 它减少 FcεRI 依赖性 Ca2+ 流入,并减少组胺、白三烯 C4 和细胞因子(IL-5/-8/-13 和 TNFα)的释放。 |
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E0137 |
GV-58
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GV-58 是一种新型的选择性 N 型和 P/Q 型 Ca2+ 通道激动剂,IC50 分别为 7.21 μM 和 8.81 μM。 |
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S5861 |
Lercanidipine
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Lercanidipine是一种对血管具有特异性的钙离子通道拮抗剂,可用于治疗发性高血压。 |
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S9842 |
MCU-i4
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MCU-i4 是 mitochondrial calcium uniporter (MCU) 复合物的负调节剂,可直接结合 MICU1 中的特定裂缝并减少线粒体 Ca2+ 流入。 |
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E2993 |
Ruthenium Red
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Ruthenium red (Ammoniated ruthenium oxychloride) 是一种聚阳离子染料,是一种L-type calcium current(ICa)阻滞剂。 它广泛用于细胞、组织和营养细菌的电子显微镜 (EM)。 Ruthenium red与磷脂和脂肪酸发生强烈反应,并与酸性粘多糖结合。 |
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S1573 |
Fasudil HCl
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Fasudil HCl是一种有效的、具有选择性的Rho抑制剂(ROCK2, Ki=0.33 μM),同时对PKA、PKG、PKC和MLCK也具有抑制活性,Ki值分别为1.6 μM、1.6 μM、3.3 μM、36 μM。Fasudil 也是calcium channel的阻滞剂。 |
- J Immunother Cancer, 2024, 12(11)e009805
- Sci China Life Sci, 2024, 67(8):1549-1562
- CNS Neurosci Ther, 2024, 30(11):e70098
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S1811 |
Amiloride HCl
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Amiloride HCl是一种选择性的T-type calcium channel阻滞剂,epithelial sodium channel(ENaC)阻滞剂,urokinase plasminogen activator (uPA)抑制剂,Ki=7 μM。 |
- J Extracell Vesicles, 2024, 13(4):e12426
- J Extracell Vesicles, 2024, 13(4):e12426
- Virus Res, 2024, 339:199258
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S4202 |
Verapamil HCl
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Verapamil HCl是L-型钙通道抑制剂,是第四类抗心律失常的药剂。Verapamil 可抑制 permeability-glycoprotein (P-gp) 和 CYP3A4。 |
- J Immunother Cancer, 2024, 12(11)e009805
- NPJ Precis Oncol, 2024, 8(1):94
- Int J Mol Sci, 2024, 25(18)10162
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S1808 |
Nifedipine
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Nifedipine是一种二氢吡啶类钙离子通道阻滞剂,是有效的血管扩张剂,具有钙拮抗作用。 |
- J Immunother Cancer, 2024, 12(11)e009805
- Laryngoscope Investig Otolaryngol, 2023, 8(5):1390-1400
- Oncogene, 2021, 40(6):1128-1146
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S2721 |
Nilvadipine
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Nilvadipine (ARC029, FR34235,FK235) 是一种强效钙通道阻滞剂,IC50为0.03 nM。 |
- J Immunother Cancer, 2024, 12(11)e009805
- Nat Commun, 2022, 13-1:6117
- J Pers Med, 2022, 12(2)258
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S2030 |
Flunarizine 2HCl
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Flunarizine 2HCl (KW-3149, R14950) 是一种二氢盐酸盐,抑制钙离子通道,Ki为68 nM。 |
- Sci Adv, 2023, 9(15):eadf2695
- J Pers Med, 2022, 12(2)258
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
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S1905 |
Amlodipine
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Amlodipine (UK-48340) 是一种长效的钙离子通道抑制剂,用于降低血压缓解胸部疼痛。 |
- J Immunother Cancer, 2024, 12(11)e009805
- Cancer Med, 2024, 13(11):e7291
- Acta Pharm Sin B, 2023, 13(10):4217-4233
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S6657 |
2-APB (2-Aminoethyl Diphenylborinate)
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2-APB (2-Aminoethyl Diphenylborinate)是IP3 receptor的抑制剂,可以调节IP3诱导的钙释放。2-APB还可以抑制SOC通道的活性,并且在高浓度的时候可以激活TRP通道。 |
- iScience, 2024, 27(8):110507
- Mol Med Rep, 2024, 30(6)220
- PLoS Pathog, 2023, 19(3):e1011295
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S1293 |
Cilnidipine
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Cilnidipine是一种L型和N型钙离子通道抑制剂,用来治疗高血压。 |
- J Immunother Cancer, 2024, 12(11)e009805
- Nat Commun, 2021, 12(1):3907
- Cell Discov, 2020, 6(1):96
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S1748 |
Nisoldipine
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Nisoldipine (Sular, BAY K 5552)是特定L型CaV1.2钙通道阻断剂,IC50为10 nM。 |
- J Immunother Cancer, 2024, 12(11)e009805
- Biomed Pharmacother, 2022, 145:112432
- iScience, 2022, 25(10):105068
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S1356 |
Levetiracetam (UCB-L059)
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Levetiracetam (UCB-L059, SIB-S1) 是一种抗癫痫化合物。Levetiracetam (UCB-L059, SIB-S1) 是 muscarinic acetylcholine receptors (mAChR) 的激动剂并能调节突触前P/Q型压敏钙离子通道 calcium (Ca2+) channel。 |
- Front Neurosci, 2023, 17:1336026
- bioRxiv, 2023, 2023.11.10.566574
- Alzheimers Dement (N Y), 2022, 8(1):e12329
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S8380 |
YM-58483 (BTP2)
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YM-58483/BTP2是钙池调控钙离子进入(SOCE)的阻滞剂,参与调解不可兴奋细胞如淋巴细胞的激活。 |
- Cell Death Discov, 2023, 9(1):100
- Dev Cell, 2022, S1534-5807(21)01035-2
- J Innate Immun, 2022, 1-13
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S1662 |
Isradipine
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Isradipine (PN 200-110)是一种高效选择性的L型压力控式钙离子通道抑制剂,用于治疗高血压。 |
- J Cell Sci, 2022, 135(14)jcs260249
- Environ Toxicol Chem, 2021, 10.1002/etc.5018
- Cell Discov, 2020, 6(1):96
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S2114 |
Dronedarone HCl
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Dronedarone HCl (SR33589) 用于治疗阵发性和持续性房颤或房扑的患者。 |
- Cancers (Basel), 2022, 14(19)4883
- Chem Res Toxicol, 2021, 10.1021/acs.chemrestox.1c00127
- Cell Syst, 2019, 8(2):97-108
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S1813 |
Amlodipine Besylate
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Amlodipine Besylate是一种长效的钙离子通道抑制剂,IC50为1.9 nM。 |
- Front Pharmacol, 2022, 13:902305
- Cell Discov, 2020, 6(1):96
- Oncogene, 2019, 38(1):120-139
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S1425 |
Ranolazine 2HCl
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Ranolazine 2HCl (RS-43285,RS 43285-193,Ranexa, renolazine,Ranolazine dihydrochloride)是一种钙离子通过 sodium/calcium channal摄取的抑制剂抗心绞痛药物,用于治疗慢性心绞痛。 |
- J Immunother Cancer, 2024, 12(11)e009805
- Basic Clin Pharmacol Toxicol, 2023, 133(2):194-201
- Cell Rep, 2022, 41(1):111445
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S2482 |
Manidipine 2HCl
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Manidipine 2HCl (CV-4093) 是Manidipine的盐酸盐形式,是钙通道阻断剂,IC50为2.6 nM,临床上常用于抗高血压。Phase 4。 |
- Adv Sci (Weinh), 2023, 10(11):e2205500
- Front Microbiol, 2023, 14:1177391
- Environ Toxicol Chem, 2021, 10.1002/etc.5018
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S1885 |
Felodipine
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Felodipine (CGH-869) 是一种选择性L型Ca2+通道阻断剂,IC50为0.15 nM。 |
- J Immunother Cancer, 2024, 12(11)e009805
- Bioact Mater, 2022, 14:272-289
- Cell Discov, 2020, 6(1):96
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S1747 |
Nimodipine
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Nimodipine (BAY E 9736) 是一种二氢吡啶衍生物,是钙离子通道抑制剂Nifedipine的类似物,具有降压活性。Nimodipine能减少细胞内游离Ca2+,Beclin-1及细胞自噬。 |
- J Immunother Cancer, 2024, 12(11)e009805
- Eye Vis (Lond), 2024, 11(1):37
- Cell Discov, 2020, 6(1):96
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S2017 |
Benidipine HCl
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Benidipine HCl (KW-3049,(±)- Benidipine) 是Benidipine的盐酸盐形式,是一种二氢吡啶类的钙离子通道抑制剂。 |
- J Immunother Cancer, 2024, 12(11)e009805
- Cell Discov, 2020, 6(1):96
- ACS Infect Dis, 2020, acsinfecdis.0c00486
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S3931 |
Ginsenoside Rd
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Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively. |
- Drug Des Devel Ther, 2022, 16:2767-2782
- J Ginseng Res, 2022, 46(5):700-709
- J Ethnopharmacol, 2021, S0378-8741(21)00169-0
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S1799 |
Ranolazine
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Ranolazine (CVT 303, RS 43285-003)是一种钙离子通过 sodium/calcium channal摄取的抑制剂抗心绞痛药物,用于治疗慢性心绞痛。 |
- Sci Rep, 2023, 10.1038/s41598-023-47540-8
- Cancer Cell, 2022, S1535-6108(22)00312-9
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S4181 |
Nicardipine HCl
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Nicardipine HCl (RS-69216,YC-93)是二氢吡啶的钙通道抑制剂,具有显著的血管扩张作用。 |
- Cell Discov, 2020, 6(1):96
- ACS Infect Dis, 2020, acsinfecdis.0c00486
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S3053 |
Azelnidipine
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Azelnidipine (UR-12592)是一种二氢吡啶类钙通道阻断剂。 |
- Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X
- Environ Toxicol Chem, 2021, 10.1002/etc.5018
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S1865 |
Diltiazem HCl
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Diltiazem (Tiazac, RG 83606) HCl 是一种Benzothiazepine衍生物,具有舒张血管的作用,由于其抑制钙离子在膜的功能。 |
- J Immunother Cancer, 2024, 12(11)e009805
- J Cell Mol Med, 2018, 22(12):5964-5977
- FASEB J, 2017, 31(2):625-635
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S4648 |
Dantrolene sodium hemiheptahydrate
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Dantrolene sodium hemiheptahydrate (Dantrium) 是一种骨骼肌松弛药,通过干扰肌纤维中的兴奋-收缩偶联起作用。 |
- Cardiovasc Res, 2021, 117(4):1091-1102
- Oxid Med Cell Longev, 2021, 2021:8810698
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S6847 |
ML-9 HCl
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ML-9 HCl (ML-9 hydrochloride) 是一种有效的选择性的 Akt kinase、myosin light chain kinase (MLCK) 和 stromal interaction molecule 1 (STIM1)。ML-9 HCl 也是 Ca2+-permeable channels 的有效抑制剂。ML-9 HCl 是一种靶向自噬和细胞死亡的亲溶酶体剂。 |
- PLoS Pathog, 2023, 19(3):e1011295
- J Mol Endocrinol, 2019, 63(3):199-213
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S2481 |
Manidipine
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Manidipine(CV-4093,(±)-Manidipine)是一种二氢吡啶类钙拮抗剂,用于治疗高血压。 |
- J Immunother Cancer, 2024, 12(11)e009805
- Antiviral Res, 2018, 150:130-136
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S2080 |
Clevidipine Butyrate
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Clevidipine Butyrate(Cleviprex)是一种二氢吡啶类钙离子通道抑制剂,用于降血压。 |
- J Immunother Cancer, 2024, 12(11)e009805
- ACS Infect Dis, 2020, acsinfecdis.0c00486
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S2573 |
Tetracaine HCl
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Tetracaine HCl (Amethocaine hydrochloride)是Tetracaine的盐酸盐形式,是一种有效的局部麻醉剂和通道功能变构酶抑制剂。 |
- PLoS Pathog, 2023, 19(3):e1011295
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S5255 |
Nicardipine
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Nicardipine is a potent calcium channel blockader with marked vasodilator action. |
- Cell Chem Biol, 2021, S2451-9456(21)00442-6
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S4626 |
Ethosuximide
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Ethosuximide(Zarontin)是一种琥珀酰亚胺类的抗痉挛试剂,主要用于失神发作。是钙离子通道阻滞剂。 |
- Nature, 2018, 554(7692):317-322
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S5966 |
Amlodipine maleate
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Amlodipine (Amvaz, UK-48340) maleate 是一种长效的 calcium channel 的阻滞剂,可用于降低血压或预防胸痛。 |
- Front Pharmacol, 2022, 13:902305
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S4597 |
Lercanidipine hydrochloride
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Lercanidipine是二氢吡啶类的钙离子通道抑制剂。 |
- J Immunother Cancer, 2024, 12(11)e009805
- J Phys Chem B, 2013, 117(23):6868-73
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S4977 |
Efonidipine
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Efonidipine (NZ-105) 是一种L型和T型钙离子通道阻滞剂,可引起血管舒张和心脏自律性降低。它还能抑制醛固酮从肾上腺分泌。 |
- Biomol Ther (Seoul), 2022, 30(5):455-464
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S6834 |
Zegocractin (CM 4620)
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Zegocractin (CM 4620)是一种 calcium-release activated calcium-channel (CRAC channel) 的抑制剂。CM4620 抑制Orai1/STIM1介导的Ca2+电流和Orai2/STIM1介导的电流,对应的IC50值分别接近120 nM和900 nM。 |
- Elife, 2023, 12e81288
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S5514 |
Lanthanum(III) chloride heptahydrate
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Lanthanum(III) chloride is the inorganic compound used in biochemical research to block the activity of divalent cation channels, mainly calcium channels. |
- J Surg Res, 2021, 263:236-244
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S3766 |
Tanshinone IIA sulfonate sodium
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Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA isolated as the main pharmacologically active natural compound from a traditional Chinese herbal medicine, the dried root of Salvia miltiorrhiza Bunge known as Danshen. Sodium tanshinone IIA sulfonate (STS) is a potent negative allosteric modulator of the human purinergic receptor P2X7. Sodium tanshinone IIA sulfonate (STS) inhibits the activity of CYP3A4 and store-operated Ca2+ entry (SOCE) through store-operated Ca2+ channels (SOCC) via downregulating the expression of transient receptor potential canonical proteins (TRPC). |
- J Inflamm Res, 2022, 15:6293-6306
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S3674 |
Levamlodipine
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Levamlodipine (S-amlodipine) is a pharmacologically active enantiomer of amlodipine which belongs to the dihydropyridine group of calcium channel blocker. It acts on the L-type of calcium channels and its treatment results in vasodilation and a fall in blood pressure. |
- Oncogene, 2021, 40(6):1128-1146
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S4727 |
Cinnarizine
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Cinnarizine (Stugeron, Dimitronal, Stutgin, Cinarizine)是piperazine的药物衍生物,是抗组胺剂和钙离子通道阻滞剂。 |
- Sci Adv, 2022, 8(15):eabk2376
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S1994 |
Lacidipine
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Lacidipine (GX-1048, GR-43659X, SN-305)是一种L-型钙离子通道抑制剂。 |
- J Immunother Cancer, 2024, 12(11)e009805
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S2491 |
Nitrendipine
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Nitrendipine (Bayotensin) 是一种二氢吡啶类钙离子通道抑制剂,IC50为95 nM。 |
- Nat Commun, 2024, 15(1):8708
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S0000 |
Cav 2.2 blocker 1
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Cav 2.2 blocker 1 (compound 9) 是一种 N-type calcium channel (Cav 2.2) 阻滞剂可用于治疗疼痛,其IC50值为0.001 μM。 |
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E0778 |
o-3M3FBS
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O-3M3FBS是m-3M3FBS的阴性对照,以独立于PLC的机制及拮抗的方式抑制内向和外向电流,可逆地抑制延迟整流K+通道,以与m-3M3FBS竞争的形式增加[Ca2+](i)。 |
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E1259 |
DNQX
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DNQX是一种AMPA受体拮抗剂,可通过电压门控钙通道防止过多的钙流入。 |
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S3045 |
Cinepazide maleate
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Cinepazide maleate是cinepazide的马来酸盐形式,而cinepazide是一种血管舒张药。 |
- J Immunother Cancer, 2024, 12(11)e009805
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S3242 |
Loureirin B
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Loureirin B (LB, LrB),是从Dracaena cochinchinensis中提取的类黄酮,是 PAI-1 的抑制剂,其IC50值为26.10 μM。Loureirin B 可下调TGF-β1刺激的成纤维细胞中的 p-ERK 和 p-JNK。Loureirin B 主要通过增加Pdx-1、MafA、细胞内ATP水平来促进胰岛素分泌,抑制 KATP 电流,Ca2+ 进入细胞内。 |
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E1879New |
CBD3063
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CBD3063(EX-A8428) 是一种选择性、同类首创的 Cav2.2-CRMP2(ollapsin 反应介质蛋白 2)相互作用抑制剂。它可抑制 Cav2.2 和 N 型(Cav2.2)钙电流的表面运输。CBD3063 变构调节 Cav2.2 以实现镇痛和缓解疼痛,且无不良副作用。 |
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S0535 |
FK962
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FK962是FK960的衍生物,具有抗痴呆的特性,在1-1000 nM时,显著增强高K+诱导的大鼠海马片的生长抑素释放,在1-100 nM时,也显著降低生长抑素诱导的大鼠海马神经元的Ca2+通道抑制。 |
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S5279 |
Fendiline hydrochloride
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Fendiline hydrochloride is the hydrochloride salt form of Fendiline, which is an L-type calcium channel blocker and also a specific inhibitor of K-Ras plasma membrane targeting with no detectable effect on the localization of H- and N-Ras. |
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S3845 |
Panaxadiol
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Panaxadiol (20(R)-Panaxadiol) is a triterpene sapogenin originally found in species of Panax (ginseng) and exhibits anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities. It inhibits Ca2+ channels, decreasing channel open time and open state probability in vitro and displaying anti-arrhythmic potential. |
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S5898 |
Efonidipine hydrochloride monoethanolate
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Efonidipine (NZ-105) hydrochloride monoethanolate 是一种L型和T型 calcium channel 的阻滞剂,可导致血管舒张并降低心脏的自动节律性。Efonidipine hydrochloride monoethanolate 还抑制肾上腺醛固酮的分泌。 |
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S3700 |
DHBP dibromide
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DHBP (1,1'-diheptyl-4,4'-bipyridinium),一种用于电致色记忆显示剂的紫罗碱,抑制由2 mM咖啡因和2 μg/ml多熔素诱导的钙释放,IC50分别为5 μg/ml和4 μg/ml。 |
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E1368 |
PD173212
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PD173212(Compound 11) 是一种选择性N 型电压敏感钙通道 (N-type voltage sensitive calcium channel, VSCC) 阻滞剂,在 IMR-32 测定中的 IC50 为 36 nM。 |
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S9017 |
Columbianadin
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Columbianadin (Zosimin, 2-Butenoic acid) 是一种来自当归的天然香豆素,已知具有多种生物活性,包括钙通道阻断活性、对各种癌细胞系的细胞毒活性、镇痛活性、肠道吸收和运输、抗炎和抗癌作用。 |
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S2403 |
Tetrandrine
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Tetrandrine是来源于千金藤根部的一种双苯基异喹啉,一种钙离子通道抑制剂。 |
- Pharmacol Res, 2024, 207:107314
- mBio, 2024, e0228723.
- Int J Mol Sci, 2024, 25(22)12330
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S9315 |
Praeruptorin A
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Praeruptorin A, a naturally existing pyranocumarin, is isolated from the dried root of Peucedanum praeruptorum Dunn. Praeruptorin A inhibits p38/Akt-c-Fos-NFATc1 signaling and PLCγ-independent Ca2+ oscillation. Praeruptorin A can significantly upregulates multidrug resistance-associated protein 2 expression via the constitutive androstane receptor-mediated pathway in vitro, and this should be taken as an herb-drug interaction. |
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S6920 |
SEA0400
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SEA0400 是一种选择性的 Na+-Ca2+ exchanger (NCX) 的强效抑制剂,可抑制神经细胞、星形胶质细胞和小胶质细胞中Na+依赖性的Ca2+吸收,对应的IC50值分别为33 nM、5.0 nM和8.3 nM。SEA0400 可防止硝普钠 (SNP) 提高 ERK 和 p38 MAPK 的磷酸化和通过细胞外Ca2+依赖的方式增强reactive oxygen species (ROS) 的产生。 |
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S4084 |
Lomerizine 2HCl
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Lomerizine dihydrochloride (KB-2796) 是一种相对较新的L-和T-型钙通道阻滞剂,用于治疗偏头痛。 |
- Nat Commun, 2024, 15(1):8708
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E0826 |
Levamlodipine Besylate
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Levamlodipine Besylate是一种强大的二氢吡啶钙通道(dihydropyridine calcium channel)阻滞剂,具有血管舒张特性,用于高血压和心绞痛的治疗。 |
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S3682 |
Ethyl 3-Aminobenzoate methanesulfonate
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Ethyl 3-Aminobenzoate (Ethyl m-Aminobenzoate, NSC 93790, Tricaine) 可通过voltage-dependent Na+-channels阻止动作电位的产生,常用于鱼类的麻醉、镇静和安乐死。 |
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E0334 |
BAMB-4
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BAMB-4 (ITPKA-IN-C14)是一种新型的膜透性的肌醇三磷酸3-激酶A(Inositol-Trisphosphate 3-Kinase A, ITPKA)抑制剂,在ADP-Glo激酶检测中,IC50为37 μM。 |
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S9400 |
Rhynchophylline
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Rhynchophylline (Mitrinermine), an active component isolated from species of the genus Uncaria, acts as a calcium channel blocker and is widely used in traditional Chinese medicine mainly for treating ailments of central nervous and cardiovascular systems, such as lightheadedness, convulsions, numbness, and hypertension. |
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S3883 |
Protopine
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Protopine (Corydinine, Fumarine, Biflorine, Macleyine), an alkaloid present in different plants, has been shown to exhibit a number of activities, such as inhibition of calcium influx through both voltage and receptor-operated channels and inhibition of rabbit blood platelet aggregation. It also possesses anti-cholinergic and anti-histaminic as well as anti-bacterial activities. |
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S5567 |
Trimethadione
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Trimethadione is an oxazolidinedione anticonvulsant and often used to treat epileptic conditions that are resistant to other treatments. |
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S9566 |
Bepridil hydrochloride
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Bepridil hydrochloride(CERM 1978)是一种抗心绞痛的药物,是钙离子通道(calcium channel)阻滞剂。它能阻止多种其他离子通道,包括钠离子和钾离子通道。 |
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S0452 |
NP118809
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NP118809(39-1B4)是一种有效的N型钙通道(N-type calcium channel)阻滞剂,IC50为0.11 μM,对L型钙通道(L-type calcium channel)的抑制作用也较弱,IC50为12.2 μM。 |
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S2975 |
CarboxyaMidotriazole orotate
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Carboxyamidotriazole Orotate (L-651582 Orotate)是Carboxyamidotriazole (CAI)的乳清酸盐形式,它是一种口服生物可利用的信号转导抑制剂。Carboxyamidotriazole Orotate是一种非电压操作的钙通道和钙通道介导的信号通路的细胞抑制抑制剂。 Carboxyamidotriazole Orotate能够抑制肿瘤生长、侵袭、转移和血管生成。 |
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S0016 |
SN-6
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SN-6 是一种选择性的 Na+/Ca2+ exchanger (NCX) 抑制剂。SN-6 可抑制NCX1、NCX2和NCX3,对应的IC50值分别为2.9 μM、16 μM和8.6 μM。SN-6 可消除 acetylcholine (ACh) 诱导的血管舒张。 |
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S6473 |
Pinaverium bromide
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Pinaverium bromide (Icosapentaenoic acid)是calcium channel阻滞剂,适用于治疗功能性胃肠病。 |
- Cell Rep, 2024, 43(11):114952
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E2984 |
GSK-7975A
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GSK-7975A 是一种有效的口服 CRAC 通道抑制剂。 它减少 FcεRI 依赖性 Ca2+ 流入,并减少组胺、白三烯 C4 和细胞因子(IL-5/-8/-13 和 TNFα)的释放。 |
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S9842 |
MCU-i4
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MCU-i4 是 mitochondrial calcium uniporter (MCU) 复合物的负调节剂,可直接结合 MICU1 中的特定裂缝并减少线粒体 Ca2+ 流入。 |
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E2993 |
Ruthenium Red
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Ruthenium red (Ammoniated ruthenium oxychloride) 是一种聚阳离子染料,是一种L-type calcium current(ICa)阻滞剂。 它广泛用于细胞、组织和营养细菌的电子显微镜 (EM)。 Ruthenium red与磷脂和脂肪酸发生强烈反应,并与酸性粘多糖结合。 |
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