Forskolin (Colforsin)

別名: HL 362, Coleonol 中文名稱：佛司可林

此產品請避光密封保存。

目錄號：S2449 Purity: 99.06%

Forskolin (Colforsin)在各種各樣細胞類型中，是一種普遍存在的真核細胞腺苷酸環(huán)化酶（AC）激活劑，在細胞生理學研究中，通常用來提高cAMP水平。Forskolin 還可激發(fā) PXR 和 FXR的活性而誘導自噬。

Forskolin (Colforsin) Chemical Structure

CAS: 66575-29-9

規(guī)格	價格	庫存
10mM (1mL in DMSO)	737.1	現(xiàn)貨
10mg	903.37	現(xiàn)貨
50mg	3029.97	現(xiàn)貨
100mg	4679.71	現(xiàn)貨
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產品質控

批次：純度： 99.06%

99.06

常與Forskolin (Colforsin)一起在實驗中被使用的化合物

SQ22536

SQ22536 抑制毛喉素引起的 cAMP 含量和腺苷酸環(huán)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環(huán)化酶后，VPA 顯著降低苔蘚纖維傳輸?shù)?PKA 依賴性增強。

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

RepSox (E-616452)

RepSox 和 Forskolin 以及其他化學混合物一起用于 iPSC 的重編程和化學誘導。

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將人尿細胞直接轉化為神經元，無需引入轉錄因子或 miRNA。

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

EPZ004777

EPZ004777 和 Forskolin 與其他小分子組合使用，作為培養(yǎng)基中的混合物，將小鼠成纖維細胞直接重編程為 ciNCC 和 ciCEC。

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

Forskolin (Colforsin)相關產品

相關靶點	AC EPAC1 EPAC2 PACAP receptor	點擊展開
相關產品	SQ22536 ESI-09 PACAP 1-38 Bithionol PACAP 6-38 acetate HJC0350	點擊展開
相關化合物庫	FDA藥物庫天然產物庫已知活性藥物庫-I GPCR小分子化合物庫	點擊展開

細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻信息
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
點擊查看更多細胞系數(shù)據(jù)

生物活性

產品描述

靶點

Adenylyl cyclase (AC) ^[1]
(A wide variety of cell types)

體外研究(In Vitro)
體外研究活性	Forskolin可以使膜，細胞或組織制備液中cAMP含量上升。Forskolin 不僅可以活化AC 而且可以與某些其它蛋白相互作用，包括葡萄糖轉運蛋白和離子通道。Forskolin能夠促進9種不同獨立AC形式的活化，雖然對AC9效率有點低，這可以用于提供一種鑒定和量化G蛋白 (G_s)–AC復合物高親和性結合位點的方法。G蛋白偶聯(lián)受體活化G蛋白有助于細胞中Forskolin刺激的cAMP 產生，因為 G蛋白-Forskolin對AC活性有增強作用^[1]。 Forskolin在不與細胞表面受體相互作用前提下刺激腺苷酸環(huán)化酶活性。在脂肪細胞中Forskolin's促進 cAMP產生進而可以抑制嗜堿性粒細胞和肥大細胞脫顆粒作用以及組胺釋放，降低血壓、眼內壓，抑制血小板聚集，促進血管舒張，支氣管擴張和甲狀腺激素分泌，刺激脂肪分解。Forskolin 抑制血小板活化因子 (PAF)的結合, 這種抑制不依賴于cAMP形成可能是 Forskolin's 直接作用于 PAF或者通過干擾PAF與它的受體結合實現(xiàn)的。Forskolin似乎對多種膜轉運蛋白也有效果并且可以抑制脂肪細胞，紅細胞，血小板，和其他細胞中的葡萄糖運輸。Forskolin也被用于治療青光眼^[2]。
實驗圖片	檢測方法	檢測指標	實驗圖片	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
臨床試驗信息 (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 - H?pitaux 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	--

參考文獻
[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. + 展開

參考文獻

[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.

+ 展開

化學信息&溶解度

分子量	410.5	分子式	C₂₂H₃₄O₇
CAS號	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
儲存條件(自收到貨起)	3年 -20°C(避光) 粉狀 1年 -80°C(避光) 溶于溶劑	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年 -20°C(避光) 粉狀 1年 -80°C(避光) 溶于溶劑	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 40 mg/mL ( (97.44 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 20 mg/mL (48.72 mM)

Water : Insoluble

DMSO : 82 mg/mL ( (199.75 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 82 mg/mL (199.75 mM)

Water : Insoluble

摩爾濃度計算器

體內溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

動物體內配方計算器

實驗計算

摩爾濃度計算器

質量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

技術支持

在訂購、運輸、儲存和使用我們的產品的任何階段，您遇到的任何問題，均可以通過撥打我們的熱線電話400-668-6834，或者技術支持郵箱tech@selleck.cn，直接聯(lián)系到我們。我們會在24小時內盡快聯(lián)系您。

操作手冊

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* 必填項

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):

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