HCV Protease

HCV Protease产品

  • 所有产品(26)
  • HCV Protease抑制剂 (26)
目录号 产品名 产品描述 文献引用 实验数据
S1482 Daclatasvir (BMS-790052) Daclatasvir (BMS-790052, EBP883) 是一种高度选择性的HCV NS5A抑制剂,EC50为9-50 pM,在细胞培养中,作用于多种HCV复制基因型和JFH-1基因型2a的感染性病毒。Phase 3。
J Med Virol, 2024, 96(7):e29787
EMBO Mol Med, 2024, 16(4):870-884
J Virol, 2024, e0192123.
S1538 Telaprevir Telaprevir是一种丙型肝炎病毒(HCV)NS3-4A丝氨酸蛋白酶抑制剂,IC50为0.354 μM。
J Virol, 2024, e0192123.
bioRxiv, 2023, 2023.11.22.568224
NPJ Digit Med, 2022, 5(1):83
S2794 Sofosbuvir Sofosbuvir是一种 HCV的NS5B polymerase抑制剂,用于治疗慢性丙型肝炎病毒(HCV)的感染。
J Med Virol, 2024, 96(7):e29787
PLoS One, 2024, 19(5):e0303265
mBio, 2023, 10.1128/mbio.01318-23
S1480 Lomibuvir (VX-222) Lomibuvir (VX-222, VCH-222)是一种新型的,有效的,选择性的HCV聚合酶抑制剂,IC50为0.94-1.2 μM,作用于突变型M423T效果低15.3倍,作用于突变型I482L效果低108倍。Phase 2。
Cell Death Discov, 2022, 8(1:446)
J Virol, 2022, jvi0190621
Sci Rep, 2021, 11(1):19443
S1183 Danoprevir Danoprevir 是一种肽类抑制剂,作用于丙型肝炎病毒(HCV)的NS3/4A蛋白酶IC50为0.2-3.5 nM,抑制HCV 1A/1B/4/5/6基因型比抑制2B/3A基因型效果高10倍左右。Phase 2。
Antimicrob Agents Chemother, 2024, 68(4):e0137323.
Viruses, 2023, 15(4)981
Cell Rep Methods, 2023, 3(10):100599
S3733 Boceprevir Boceprevir (EBP 520, SCH 503034)是一种口服的、直接作用于hepatitis C virus (HCV) protease的抑制剂,对NS3蛋白酶的Ki值为14 nM。在治疗慢性肝炎C(genotype 1)中,常与其他抗病毒共同给药。
Eur J Med Chem, 2024, 268:116202
Int J Mol Sci, 2024, 25(11)5767
SLAS Discov, 2024, S2472-5552(24)00043-1
S5062 Daclatasvir Dihydrochloride Daclatasvir是一种具有口服活性的抗病毒剂,抑制HCVNS5A区域,用于治疗慢性遗传型1和3类的HCV感染。
Commun Biol, 2022, 5(1):154
J Antimicrob Chemother, 2021, 76(7):1874-1885
Med Mol Morphol, 2021, 10.1007/s00795-020-00271-5
S7579 Ledipasvir (GS5885) Ledipasvir (GS5885) 是一种HCV NS5A polymerase抑制剂,用于治疗丙型肝炎病毒感染。
Sci Rep, 2021, 11(1):19443
Cancers (Basel), 2019, 11(10)E1407
Biol Pharm Bull, 2019, 10.1248/bpb.b19-00641
S5015 Simeprevir Simeprevir一种竞争性的、可逆的、非共价结合的大环hepatitis C virus (HCV) NS3/4A protease抑制剂,直接抑制HCV病毒。它对HCV NS3/4A(genotypes 1a, 1b, 2, 4, 5, and 6)的平均IC50值小于13 nM,而对genotype 3的IC50值为37 nM。
Chemistry, 2022, e202202798.
Cell Rep, 2021, 35(7):109133
Viruses, 2021, 13(2)173
S4935 Asunaprevir Asunaprevir是具有口服活性的HCV NS3抑制剂。HCV NS3是病毒复制蛋白加工所必需的蛋白酶。
Int J Mol Sci, 2023, 10.3390/ijms242115535
Nature, 2022, 604(7904):146-151
Chemistry, 2022, e202202798.
S3728 Grazoprevir Grazoprevir anhydrous (MK5172) 是一种 Hepatitis C Virus NS3/4A Protease 的抑制剂,HCV genotype 1a、1B和4的IC50值分别为7pM、4pM和62pM。
Cell Res, 2024, 34(1):31-46
Cell Rep, 2021, 35(7):109133
Front Oncol, 2021, 11:803278
S3724 Velpatasvir Velpatasvir (GS-5816,VEL) 是二代NS5A抑制剂,抑制丙型肝炎病毒(HCV)的复制。
mBio, 2023, 10.1128/mbio.01318-23
Front Oncol, 2021, 11:803278
Front Microbiol, 2020, 10:2936
S5403 Ombitasvir (ABT-267) Ombitasvir (ABT-267)是HCV NS5A的抑制剂,具有抗病毒活性。
Commun Biol, 2022, 5(1):154
Sci Rep, 2021, 11(1):19443
bioRxiv, 2021, 2021.07.21.453274
S5402 Dasabuvir (ABT-333) Dasabuvir (ABT-333) is a non-nucleoside inhibitor of NS5B viral RNA-dependent RNA polymerase that inhibits recombinant NS5B polymerases derived from HCV genotype 1a and 1b clinical isolates with IC50 values between 2.2 and 10.7 nM. It is at least 7,000-fold selective for the inhibition of HCV genotype 1 polymerases over human/mammalian polymerases.
J Virus Erad, 2022, 8(2):100074
mSphere, 2021, 6(6):e0062321
Sci Rep, 2021, 11(1):19443
S5720 Glecaprevir
Cell Rep, 2021, 35(7):109133
Sci Rep, 2021, 11(1):19443
BioRxiv, 2020, 10.1101/2020.12.13.422511
S5404 Paritaprevir (ABT-450) Paritaprevir (ABT-450)是NS3/4A抑制剂。
Cell Rep, 2021, 35(7):109133
BioRxiv, 2020, 10.1101/2020.12.13.422511
S3800 Lycorine hydrochloride Lycorine (Galanthidine, Amarylline, Narcissine, Licorine), a natural alkaloid extracted from the Amaryllidaceae plant family, has been reported to exhibit a wide range of physiological effects, including the potential effect against cancer. It is an HCV inhibitor with strong activity.
Aging Cell, 2021, e13307
S5307 PSI-6206 (GS-331007) PSI-6206 (RO-2433, GS-331007)是有效的HCV RNA依赖性RNA聚合酶抑制剂,靶向NS5B聚合酶
J Virus Erad, 2022, 8(2):100074
S3395 Tegobuvir Tegobuvir (TGV, GS 333126, GS-9190) 是一种 HCV RNA replication 的非核苷抑制剂,在被HCV感染的患者中已证明具有抗病毒的活性。
S9641 Pibrentasvir (ABT-530) Pibrentasvir (ABT-530) 是一种新型的泛基因型丙型肝炎病毒 hepatitis C virus (HCV) NS5A 抑制剂,其针对包含基因型1至6的NS5A的HCV复制子的EC50值为1.4 pM至5.0 pM。
S5394 Tizoxanide Tizoxanide (Desacetyl-nitazoxanide), a thiazolide anti-infective, is active against anaerobic bacteria, protozoa, and a range of viruses in cell culture models, and is currently in phase II clinical development for treating chronic hepatitis C.
Mol Ther, 2024, S1525-0016(24)00340-X
Int J Mol Sci, 2024, 25(8)4413
E0097 Mericitabine Mericitabine (RG 7128, R-7128, PSI 6130 diisobutyrate)是HCV NS5B聚合酶(HCV NS5B polymerase)的核苷抑制剂,作为RNA链终止子,在复制过程中防止RNA转录本的延伸。
S5652 Elbasvir Elbasvir (MK8742) is an NS5A inhibitor, preventing hepatitis C viral RNA replication and virion assembly. Median EC50 values range from 0.2 to 3600 pmol/L, based on genotype.
E3597 Herba taxilli Extract Herba Taxilli Extract是从桑寄生Taxillus sutchuenensis中提取的,可用作HCV NS3丝氨酸蛋白酶的抑制剂。
S2074 Mecarbinate Mecarbinate (Dimecarbin) 是Arbidol Hydrochloride的化学中间体。
E1243 Azvudine Azvudine (RO-0622)是一种新型核苷类逆转录酶抑制剂,对人类免疫缺陷病毒(human immunodeficiency virus, HIV)、乙型肝炎病毒(hepatitis B virus, HBV)和丙型肝炎病毒(hepatitis C virus, HCV)具有抗病毒活性,可有效抑制HIV-1 (EC50为0.03~6.92 nM)和HIV-2 (EC50为0.018~0.025 nM)。
S1482 Daclatasvir (BMS-790052) Daclatasvir (BMS-790052, EBP883) 是一种高度选择性的HCV NS5A抑制剂,EC50为9-50 pM,在细胞培养中,作用于多种HCV复制基因型和JFH-1基因型2a的感染性病毒。Phase 3。
J Med Virol, 2024, 96(7):e29787
EMBO Mol Med, 2024, 16(4):870-884
J Virol, 2024, e0192123.
S1538 Telaprevir Telaprevir是一种丙型肝炎病毒(HCV)NS3-4A丝氨酸蛋白酶抑制剂,IC50为0.354 μM。
J Virol, 2024, e0192123.
bioRxiv, 2023, 2023.11.22.568224
NPJ Digit Med, 2022, 5(1):83
S2794 Sofosbuvir Sofosbuvir是一种 HCV的NS5B polymerase抑制剂,用于治疗慢性丙型肝炎病毒(HCV)的感染。
J Med Virol, 2024, 96(7):e29787
PLoS One, 2024, 19(5):e0303265
mBio, 2023, 10.1128/mbio.01318-23
S1480 Lomibuvir (VX-222) Lomibuvir (VX-222, VCH-222)是一种新型的,有效的,选择性的HCV聚合酶抑制剂,IC50为0.94-1.2 μM,作用于突变型M423T效果低15.3倍,作用于突变型I482L效果低108倍。Phase 2。
Cell Death Discov, 2022, 8(1:446)
J Virol, 2022, jvi0190621
Sci Rep, 2021, 11(1):19443
S1183 Danoprevir Danoprevir 是一种肽类抑制剂,作用于丙型肝炎病毒(HCV)的NS3/4A蛋白酶IC50为0.2-3.5 nM,抑制HCV 1A/1B/4/5/6基因型比抑制2B/3A基因型效果高10倍左右。Phase 2。
Antimicrob Agents Chemother, 2024, 68(4):e0137323.
Viruses, 2023, 15(4)981
Cell Rep Methods, 2023, 3(10):100599
S3733 Boceprevir Boceprevir (EBP 520, SCH 503034)是一种口服的、直接作用于hepatitis C virus (HCV) protease的抑制剂,对NS3蛋白酶的Ki值为14 nM。在治疗慢性肝炎C(genotype 1)中,常与其他抗病毒共同给药。
Eur J Med Chem, 2024, 268:116202
Int J Mol Sci, 2024, 25(11)5767
SLAS Discov, 2024, S2472-5552(24)00043-1
S5062 Daclatasvir Dihydrochloride Daclatasvir是一种具有口服活性的抗病毒剂,抑制HCVNS5A区域,用于治疗慢性遗传型1和3类的HCV感染。
Commun Biol, 2022, 5(1):154
J Antimicrob Chemother, 2021, 76(7):1874-1885
Med Mol Morphol, 2021, 10.1007/s00795-020-00271-5
S7579 Ledipasvir (GS5885) Ledipasvir (GS5885) 是一种HCV NS5A polymerase抑制剂,用于治疗丙型肝炎病毒感染。
Sci Rep, 2021, 11(1):19443
Cancers (Basel), 2019, 11(10)E1407
Biol Pharm Bull, 2019, 10.1248/bpb.b19-00641
S5015 Simeprevir Simeprevir一种竞争性的、可逆的、非共价结合的大环hepatitis C virus (HCV) NS3/4A protease抑制剂,直接抑制HCV病毒。它对HCV NS3/4A(genotypes 1a, 1b, 2, 4, 5, and 6)的平均IC50值小于13 nM,而对genotype 3的IC50值为37 nM。
Chemistry, 2022, e202202798.
Cell Rep, 2021, 35(7):109133
Viruses, 2021, 13(2)173
S4935 Asunaprevir Asunaprevir是具有口服活性的HCV NS3抑制剂。HCV NS3是病毒复制蛋白加工所必需的蛋白酶。
Int J Mol Sci, 2023, 10.3390/ijms242115535
Nature, 2022, 604(7904):146-151
Chemistry, 2022, e202202798.
S3728 Grazoprevir Grazoprevir anhydrous (MK5172) 是一种 Hepatitis C Virus NS3/4A Protease 的抑制剂,HCV genotype 1a、1B和4的IC50值分别为7pM、4pM和62pM。
Cell Res, 2024, 34(1):31-46
Cell Rep, 2021, 35(7):109133
Front Oncol, 2021, 11:803278
S3724 Velpatasvir Velpatasvir (GS-5816,VEL) 是二代NS5A抑制剂,抑制丙型肝炎病毒(HCV)的复制。
mBio, 2023, 10.1128/mbio.01318-23
Front Oncol, 2021, 11:803278
Front Microbiol, 2020, 10:2936
S5403 Ombitasvir (ABT-267) Ombitasvir (ABT-267)是HCV NS5A的抑制剂,具有抗病毒活性。
Commun Biol, 2022, 5(1):154
Sci Rep, 2021, 11(1):19443
bioRxiv, 2021, 2021.07.21.453274
S5402 Dasabuvir (ABT-333) Dasabuvir (ABT-333) is a non-nucleoside inhibitor of NS5B viral RNA-dependent RNA polymerase that inhibits recombinant NS5B polymerases derived from HCV genotype 1a and 1b clinical isolates with IC50 values between 2.2 and 10.7 nM. It is at least 7,000-fold selective for the inhibition of HCV genotype 1 polymerases over human/mammalian polymerases.
J Virus Erad, 2022, 8(2):100074
mSphere, 2021, 6(6):e0062321
Sci Rep, 2021, 11(1):19443
S5720 Glecaprevir
Cell Rep, 2021, 35(7):109133
Sci Rep, 2021, 11(1):19443
BioRxiv, 2020, 10.1101/2020.12.13.422511
S5404 Paritaprevir (ABT-450) Paritaprevir (ABT-450)是NS3/4A抑制剂。
Cell Rep, 2021, 35(7):109133
BioRxiv, 2020, 10.1101/2020.12.13.422511
S3800 Lycorine hydrochloride Lycorine (Galanthidine, Amarylline, Narcissine, Licorine), a natural alkaloid extracted from the Amaryllidaceae plant family, has been reported to exhibit a wide range of physiological effects, including the potential effect against cancer. It is an HCV inhibitor with strong activity.
Aging Cell, 2021, e13307
S5307 PSI-6206 (GS-331007) PSI-6206 (RO-2433, GS-331007)是有效的HCV RNA依赖性RNA聚合酶抑制剂,靶向NS5B聚合酶
J Virus Erad, 2022, 8(2):100074
S3395 Tegobuvir Tegobuvir (TGV, GS 333126, GS-9190) 是一种 HCV RNA replication 的非核苷抑制剂,在被HCV感染的患者中已证明具有抗病毒的活性。
S9641 Pibrentasvir (ABT-530) Pibrentasvir (ABT-530) 是一种新型的泛基因型丙型肝炎病毒 hepatitis C virus (HCV) NS5A 抑制剂,其针对包含基因型1至6的NS5A的HCV复制子的EC50值为1.4 pM至5.0 pM。
S5394 Tizoxanide Tizoxanide (Desacetyl-nitazoxanide), a thiazolide anti-infective, is active against anaerobic bacteria, protozoa, and a range of viruses in cell culture models, and is currently in phase II clinical development for treating chronic hepatitis C.
Mol Ther, 2024, S1525-0016(24)00340-X
Int J Mol Sci, 2024, 25(8)4413
E0097 Mericitabine Mericitabine (RG 7128, R-7128, PSI 6130 diisobutyrate)是HCV NS5B聚合酶(HCV NS5B polymerase)的核苷抑制剂,作为RNA链终止子,在复制过程中防止RNA转录本的延伸。
S5652 Elbasvir Elbasvir (MK8742) is an NS5A inhibitor, preventing hepatitis C viral RNA replication and virion assembly. Median EC50 values range from 0.2 to 3600 pmol/L, based on genotype.
E3597 Herba taxilli Extract Herba Taxilli Extract是从桑寄生Taxillus sutchuenensis中提取的,可用作HCV NS3丝氨酸蛋白酶的抑制剂。
S2074 Mecarbinate Mecarbinate (Dimecarbin) 是Arbidol Hydrochloride的化学中间体。
E1243 Azvudine Azvudine (RO-0622)是一种新型核苷类逆转录酶抑制剂,对人类免疫缺陷病毒(human immunodeficiency virus, HIV)、乙型肝炎病毒(hepatitis B virus, HBV)和丙型肝炎病毒(hepatitis C virus, HCV)具有抗病毒活性,可有效抑制HIV-1 (EC50为0.03~6.92 nM)和HIV-2 (EC50为0.018~0.025 nM)。

HCV Protease抑制剂选择性比较

HCV Protease信号通路图

HCV Protease信号通路图
Tags: HCV protease treatment | HCV protease assay | HCV protease inhibitors review
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