相关靶点	AC EPAC1 EPAC2 PACAP receptor	点击展开
相关产品	SQ22536 ESI-09 PACAP 1-38 Bithionol PACAP 6-38 acetate HJC0350	点击展开
相关化合物库	FDA药物库天然产物库已知活性药物库-I GPCR小分子化合物库	点击展开

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

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 (G_s)–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
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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	--

参考文献
[1] Insel PA, et al. Cell Mol Neurobiol, 2003, 23(3), 305-314. [2] Wagh VD, et al. J Postgrad Med, 2012, 58(3), 199-202. [3] Liang C, et al. Nucleic Acids Res. 2022 Apr 8;50(6):3323-3347. [4] El-Agroudy NN, et al. Br J Pharmacol. 2016 Nov;173(22):3248-3260. + 展开

参考文献

[4] El-Agroudy NN, et al. Br J Pharmacol. 2016 Nov;173(22):3248-3260.

+ 展开

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	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
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	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C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

DMSO : 82 mg/mL ( (199.75 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 82 mg/mL (199.75 mM)

Water : Insoluble

DMSO : 82 mg/mL ( (199.75 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 82 mg/mL (199.75 mM)

Water : Insoluble

DMSO : 82 mg/mL ( (199.75 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

体内溶解配方批次：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
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	1.050mg/ml (2.56mM)	以 1 mL 工作液为例，取50μL21mg/ml的澄清DMSO储备液加到400μL PEG300中，混合均匀使其澄清；向上述体系中加入50μLTween80，混合均匀使其澄清；然后继续加入500μL ddH2O定容至 1 mL。工作液请现配现用！
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	4.1mg/ml (9.99mM)	以 1 mL 工作液为例,取50μL82mg/ml的澄清DMSO储备液加到400μLPEG300中,混合均匀使其澄清;向上述体系中加入50μLTween80,混合均匀使其澄清;然后继续加入500μLddH2O定容至1mL。工作液请现配现用!
澄清溶液	5% DMSO 1 95% Corn oil 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	0.55mg/ml (1.34mM)	以1 mL工作液为例，取50μL 11mg/ml的澄清DMSO储备液加到950μL玉米油中，混合均匀。工作液请现配现用！

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

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）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

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。

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

* 必填项

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Forskolin (Colforsin)

产品质控

常与Forskolin (Colforsin)一起在实验中被使用的化合物