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Forskolin (Colforsin)

别名: HL 362, Coleonol 中文名称：佛司可林

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Forskolin (Colforsin)在各种各样细胞类型中，是一种普遍存在的真核细胞腺苷酸环化酶（AC）激活剂，在细胞生理学研究中，通常用来提高cAMP水平。Forskolin 还可激发 PXR 和 FXR的活性而诱导自噬。

Forskolin (Colforsin) Chemical Structure

Forskolin (Colforsin) Chemical Structure

CAS: 66575-29-9

规格 价格 库存 购买数量
10mM (1mL in DMSO) 737.1 现货
10mg 903.37 现货
50mg 3029.97 现货
100mg 4679.71 现货
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常与Forskolin (Colforsin)一起在实验中被使用的化合物

SQ22536

SQ22536 抑制毛喉素引起的 cAMP 含量和腺苷酸环化酶活性升高。

Gao Y, et al. Eur J Pharmacol. 2001 Apr 20;418(1-2):111-6.

VPA (Valproic acid)

用毛喉素激活腺苷酸环化酶后，VPA 显著降低苔藓纤维传输的 PKA 依赖性增强。

Chang P, et al. Epilepsia. 2010 Aug;51(8):1533-42.

RepSox (E-616452)

RepSox 和 Forskolin 以及其他化学混合物一起用于 iPSC 的重编程和化学诱导。

Xie X, et al. Curr Opin Genet Dev. 2017 Oct;46:104-113.

TTNPB

TTNPB 和 Forskolin 以及其他小分子可以将人尿细胞直接转化为神经元，无需引入转录因子或 miRNA。

Xu G, et al. Sci Rep. 2019 Nov 13;9(1):16707.

EPZ004777

EPZ004777 和 Forskolin 与其他小分子组合使用，作为培养基中的混合物，将小鼠成纤维细胞直接重编程为 ciNCC 和 ciCEC。

Pan SH, et al. Sci Adv. 2021 Jun 4;7(23):eabg5749.

Forskolin (Colforsin)相关产品

相关信号通路图

cAMP Signaling Pathways

cAMP信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
SH-SY5Y  Function Assay 10 μM 1 h  increases LUC activity 25597433
SH-SY5Y  Function Assay 10 μM 1 h  increases AGC1 mRNA level 25597433
hADSCs Function Assay 5 µM 30 min increases cAMP levels 25591908
HEK293  Function Assay 5 µM 30 min increases cAMP levels 25591908
3T3-L1 Function Assay 2.5/5 μM 24 h  significantly decreases ATGL protein expression at all doses tested 25590597
OCI-Ly1  Function Assay 40 μM 1 h  induces the increment of cAMP concentrations 25576220
OCI-Ly18  Function Assay 40 μM 1 h  induces the increment of cAMP concentrations 25576220
BeWo Function Assay 20 µM 48 h increases the differentiation of BeWo cells 25566740
BeWo Function Assay 20 µM 48 h increases the adhesion of THP-1 monocytes 25566740
LNCaP  Function Assay 10 μM 12 h  induces a dramatic increase of CREB1 activity 25548099
ThGCs  Function Assay 10 μM 4 h augments HIF1A levels that were stimulated by CoCl2 25433027
ThGCs  Function Assay 10 μM 4 h increases CoCl2-induced EDN2 gene expression 25433027
ThGCs  Function Assay 10 μM 3 h inhibits the effect of H2O2 on EDN2 mRNA 25433027
RBMECs Function Assay 0.05/0.5/5 μM 0.25 h increases cAMP concentration 25416651
RBMECs Function Assay 5 μM 1 h blocks the activation of RhoA/ROCK induced by EMAP-II 25416651
RBMECs Function Assay 5 μM 1 h prevents the EMAP-II-induced TEER value decrease 25416651
RBMECs Function Assay 5 μM 1 h prevents the increase in HRP flux across the BTB induced by EMAP-II 25416651
RBMECs Function Assay 5 μM 1 h inhibits the decreased of amount of ZO-1 in MFs induced by EMAP-II 25416651
RBMECs Function Assay 5 μM 1 h reverses the changes in ZO-1 distribution seen with EMAP-II treatment 25416651
RBMECs Function Assay 5 μM 1 h blocks the EMAP-II-induced change in MLC phosphorylation 25416651
RBMECs Function Assay 5 μM 1 h blocks the actin cytoskeleton rearrangement seen with EMAP-II treatment  25416651
Primary bovine chondrocytes Growth Inhibition Assay 5μM 48 h reverses the inhibitory effect of celecoxib on proliferation in growth plate chondrocytes 25406016
EM1  Function Assay 15 μM 48 h reduces the expression of LIF or PTGS2 in CALR- or EPAC2-silenced EM1 cells  25378661
BeWo  Function Assay 20 µM 48 h  increases the beta-hCG release 25362260
BeWo  Function Assay 20 µM 48 h  downregulates the level of TMEMF16 25362260
BeWo  Function Assay 20 µM 48 h  downregulates the level of GCM-1 25362260
granulosa cells Function Assay 10 μM 12/24 h increases the levels of RGS2 mRNA 25339105
granulosa cells Function Assay 10 μM 12/24 h increases the levels of reporter activity for the longest fragment (−854/+18RGS2.LUC) 25339105
granulosa cells Function Assay 10 μM 24 h increases the intensity of DNA/protein complex 25339105
granulosa cells Function Assay 10 μM 24 h increases the levels of RGS2 promoter activity 25339105
SK-N-AS  Cell Viability Assay 10 μM  24/48 h enhances time-dependently cellular viability  25266063
SK-N-AS  Function Assay 10 μM  24 h increases the cAMP levels  25266063
SK-N-AS  Function Assay 10 μM  24 h increases the expression of cyclin D1 25266063
SK-N-AS  Function Assay 10 μM  30 min induces phosphorylation of β-catenin (ser675), p-GSK3β (ser9) and concomitant higher levels of active, unphosphorylated, β-catenin 25266063
SK-N-AS  Function Assay 10 μM  10/30/60 min increases levels of p-β-catenin (ser675) and induces accumulation of p-β-catenin (ser675) in (peri)nuclear regions 25266063
SK-N-SH Cell Viability Assay 10 μM  48 h enhances SK-N-SH neuroblastoma cell viability 25266063
HEK‐CFTR Function Assay 2–50 μM 0-12 min induces a dose‐dependent iodide efflux  25263207
L6 Function Assay 40 µM 24 h inhibits DMH1-induced Akt activation 25247550
MIN6  Function Assay 10 μM  3 h increases D3 mRNA expression 25241124
BeWo  Function Assay 20 µM 48 h induces cell fusion 25184477
THP-1  Function Assay 1/10 μM 2 h suppresses MCP-1 production  25154882
Huh-7 Function Assay 0-20 μM 2 h  results in a dose-dependent increase in c-Myc expression at the protein and mRNA levels 25109834
C6 Function Assay 10 μM  20 min increases cAMP accumulation 25069417
SW480 Function Assay 40 μM 48 h activates PP2A 24997451
HT-29  Function Assay 40 μM 48 h activates PP2A 24997451
SW480 Growth Inhibition Assay 40 μM 0-72 h inhibits cell growth time dependently 24997451
HT-29  Growth Inhibition Assay 40 μM 0-72 h inhibits cell growth time dependently 24997451
SW480 Function Assay 40 μM 7 d reduces colonosphere formation capability  24997451
HT-29  Function Assay 40 μM 7 d reduces colonosphere formation capability  24997451
SW480 Apoptosis Assay 40 μM 48 h induces an activation of caspase 3/7 24997451
HT-29  Apoptosis Assay 40 μM 48 h induces an activation of caspase 3/7 24997451
SW480 Apoptosis Assay 40 μM 48 h induces changes in the phosphorylation status of PP2A targets 24997451
HT-29  Apoptosis Assay 40 μM 48 h induces changes in the phosphorylation status of PP2A targets 24997451
UACC-647  Function Assay 10 μM 15 min increases eEF2 phosphorylation levels  25703025
UACC-647  Function Assay 10 μM 15 min inhibits ERK phosphorylation 25703025
SC Function Assay 0.5 μM 72 h increases both Krox-20 and O1 expression in axon-related SCs but only Krox-20  25705874
SC Function Assay 0.5 μM 24 h mimicks the effect of cAMP analogs on O1 and MBP expression 25705874
oocytes Function Assay 5 μM 24 h attenuates rh-insulin action on oocyte GVBD significantly  25707854
BeWo Function Assay 10 μM  72 h mediates BeWo cell differentiation 25713425
GH3 Function Assay 1 μM 6-h induces PRL and Bmal1, but not Clock, mRNA expression 25727018
GH3 Function Assay 1 μM 6-h attenuates the correlation between PRL and Bmal1 expression 25727018
PC12 Function Assay 25 μM 48 h activates cAMP 25769305
BAECs Function Assay 25 μM 24 h enhances the activation of PPARα by 5 μM resveratrol, T4HS, or 4-PAP 25798826
GLUTag  Function Assay 10 µM 4 h increases the pCREB levels with the IBMX 25832631
GLUTag  Function Assay 10 µM 0/2/4 h stimulates GLP-1 secretion cotreated with IBMX 25832631
PBMC Function Assay 50 μM 24 h  inhibits the increased secretion of TNF induced by the DPE 25866079
H295R  Function Assay 10 μM 48 h increases steroid metabolites in the androgen, mineralo- and glucocorticoid pathways 25869556
3T3-L1 preadipocytes Function Assay 10 μM  12 h induces CREB phosphorylation and C/EBPβ expression 25928058
PCCL3 Function Assay 10 µM 24 h enhances DuOx2 promoter transcription activity ​ 25960956
PC-3 Cell Viability Assay 40 µM 24/48/72 h decreases cell viability time dependently 26023836
PC-3 Function Assay 40 µM 2 h leads to PP2A activation 26023836
SH-SY5Y Function Assay 30 μM 30 min significantly increases the activation of PKA 26025137
EndoC-βH1 Function Assay 5 μM 1 h leads to a strong cAMP increase 26028562
EndoC-βH1 Function Assay 5 μM 1 h potentiates glucose-induced insulin secretion in the presence of glucose 26028562
RBMECs Function Assay 5 μM 1 h inhibits EMAP-II-induced inactivation of Rap1  26044663
AML-12  Function Assay 20 μM 3 h induces the dephosphorylation of CRTC2  26048985
AML-12  Function Assay 20 μM 3 h up-regulates Pgc1a, Pepck, and G6pc mRNA levels 26048985
AML-12  Function Assay 20 μM 1-8 h increases glucose production 26048985
AML-12  Function Assay 20 μM 3 h upregulates the phosphorylation levels at Thr-411 and Ser-493 26048985
Caco-2  Function Assay 0.1/1/10 μM 24 h increases MRP2 protein level 26049102
Caco-2  Function Assay 0.1/1/10 μM 20 min induces a dose-dependent increase in intracellular cAMP levels 26049102
bovine oocytes Function Assay 100 μM 12 h inhibits the effect of NPPA and/or NPPC to stimulate resumption of meiosis 26051611
BeWo  Function Assay 25 μM 24/48/72 h leads to an increase in the expression of other fusion markers 26053549
Spinal cords  Function Assay 1 μM 30 min stimulates cAMP levels 26126926
MDCK  Function Assay 10 µM 24 h inhibits the increased expression of FN caused by TGF-β1 26202352
MDCK  Function Assay 10 µM 24 h upregulates the expression of TGF-β1 and CTGF  26202352
RPMI 8226 Cell Viability Assay 0-100 μM 72 h induces cell death dose dependently 26306624
H929 Cell Viability Assay 0-100 μM 72 h induces cell death dose dependently 26306624
U266 Cell Viability Assay 0-100 μM 72 h induces cell death dose dependently 26306624
OPM-2 Cell Viability Assay 0-100 μM 72 h induces cell death dose dependently 26306624
INA-6 Cell Viability Assay 0-100 μM 72 h induces cell death dose dependently 26306624
RBMECs  Function Assay 5 μM 1 h blocks the Rac1 inactivation induced by EMAP-II 26358039
Mo-DCs Function Assay 50 μM 24 h promotes IL-23 production in the supernatant of zymosan stimulated Mo-DCs  26412948
HEK293 Function Assay 10 μM 6 h increases phosphorylation of overexpressed KLHL3 at S433 26435498
epithelial cells Function assay 1 uM 4, 6, and 8 days 19966789
HEK293 Function assay 10 uM 16 hrs 26435512
ventricular cardiomyocytes  Function Assay 0.01-10 μM increases cAMP accumulation 25203113
ventricular cardiomyocytes  Function Assay 0.01-10 μM evokes an inotropic response 120±15% above basal with an EC50 of 2.2 µM 25203113
SCG Function Assay 100 μM  reduces the excitability of SCG neurons 25962132
HEK-293 Function Assay 35 μM  induces a conspicuous “inactivation” of the Kv2.1 current 25962132
SCG Function Assay 20 μM  reversibly suppresses IKV with a IC50 of 24.4 μM 25962132
HEK293T Function assay 10 uM 24387325
ASK Function assay 1 hr 2849641
HepG2 (DPX-2) Function assay 24 hrs 20966043
HepG2 Function assay 24 hrs 20966043
HepG2 (DPX-2) Function assay 24 hrs 20966043
MCF7 Cytotoxicity assay 48 hrs 28838692
HEK293 Function assay 30 mins 30006176
UACC-647  Function Assay leads to a rise in cAMP levels (EC50 = 20.39 μM) 25703025
Vero E6 Antiviral assay 17663539
点击查看更多细胞系数据

生物活性

产品描述 Forskolin (Colforsin)在各种各样细胞类型中，是一种普遍存在的真核细胞腺苷酸环化酶（AC）激活剂，在细胞生理学研究中，通常用来提高cAMP水平。Forskolin 还可激发 PXR 和 FXR的活性而诱导自噬。
靶点
Adenylyl cyclase (AC) [1]
(A wide variety of cell types)
体外研究(In Vitro)
体外研究活性

Forskolin可以使膜，细胞或组织制备液中cAMP含量上升。Forskolin 不仅可以活化AC 而且可以与某些其它蛋白相互作用，包括葡萄糖转运蛋白和离子通道。Forskolin能够促进9种不同独立AC形式的活化，虽然对AC9效率有点低，这可以用于提供一种鉴定和量化G蛋白 (Gs)–AC复合物高亲和性结合位点的方法。G蛋白偶联受体活化G蛋白有助于细胞中Forskolin刺激的cAMP 产生，因为 G蛋白-Forskolin对AC活性有增强作用[1]。

Forskolin在不与细胞表面受体相互作用前提下刺激腺苷酸环化酶活性。在脂肪细胞中Forskolin's促进 cAMP产生进而可以抑制嗜碱性粒细胞和肥大细胞脱颗粒作用以及组胺释放，降低血压、眼内压，抑制血小板聚集，促进血管舒张，支气管扩张和甲状腺激素分泌，刺激脂肪分解。Forskolin 抑制血小板活化因子 (PAF)的结合, 这种抑制不依赖于cAMP形成可能是 Forskolin's 直接作用于 PAF或者通过干扰PAF与它的受体结合实现的。Forskolin似乎对多种膜转运蛋白也有效果并且可以抑制脂肪细胞，红细胞，血小板，和其他细胞中的葡萄糖运输。Forskolin也被用于治疗青光眼[2]。
实验图片 检测方法 检测指标 实验图片 PMID
Western blot cleaved caspase-3 / caspase-3 cleaved caspase-9 / caspase-9 β-catenin c-myc / Cyclin D1 pS6K1 / S6K1 / pCREB / CREB p-JNK / JNK / P-p38 / p38 30863177
Immunofluorescence 5hmC Fe(II) CYP17A1 / CYP21A2 29239726
Growth inhibition assay Cell viability 30863177
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04254705 Withdrawn
Cystic Fibrosis
Universitaire Ziekenhuizen KU Leuven|Vertex Pharmaceuticals Incorporated|KU Leuven|University of Lisbon
 March 1 2020 Not Applicable
NCT02807415 Completed
Cystic Fibrosis
Hannover Medical School|Heidelberg University|University of Giessen
 June 1 2016 --
NCT02586883 Completed
Idiopathic Dilation of the Bronchi
Assistance Publique - Hôpitaux de Paris
 March 29 2016 Not Applicable
NCT03652090 Completed
Cystic Fibrosis
Institut National de la Santé Et de la Recherche Médicale France|ABCF2
 September 1 2010 --

化学信息&溶解度

分子量 410.5 分子式

C22H34O7
CAS号 66575-29-9 SDF Download Forskolin (Colforsin) SDF
Smiles CC(=O)OC1C(C2C(CCC(C2(C3(C1(OC(CC3=O)(C)C=C)C)O)C)O)(C)C)O
储存条件(自收到货起) 3年 -20°C(避光) 粉状
1年 -80°C(避光) 溶于溶剂

体外溶解度
批次：

DMSO : 40 mg/mL ( (97.44 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 20 mg/mL (48.72 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

 动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

mg/kg g μL 只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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