Forskolin (Synonyms: 毛喉素; Coleonol; Colforsin; HL 362)

目录号: HY-15371G: Data Sheet 产品使用指南
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Forskolin (Coleonol) (GMP) 是一种有效的腺苷酸环化酶 (adenylate cyclase) 激活剂，对于 I 型腺苷酸环化酶，IC₅₀ 为 41 nM，EC₅₀ 为 0.5 μM。Forskolin (GMP) 也是一种细胞内 cAMP 形成的诱导剂。Forskolin (GMP) 诱导多种细胞类型的分化并激活孕烷 X 受体 (PXR) 和 FXR。Forskolin (GMP) 对心脏产生正性肌力作用，并具有血小板抗凝集和降压作用。Forskolin (GMP) 也可诱导细胞自噬 (autophagy)。

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Forskolin Chemical Structure

CAS No. : 66575-29-9

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生物活性
纯度 & 产品资料
参考文献

生物活性

Forskolin (Coleonol) (GMP) is a potent adenylate cyclase activator with an IC₅₀ of 41 nM and an EC₅₀ of 0.5 μM for type I adenylyl cyclase^[1]. Forskolin (GMP) is also an inducer of intracellular cAMP formation^[2]. Forskolin (GMP) induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR^[3]. Forskolin (GMP) exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin (GMP) also induces autophagy^[4]^[5].

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
BT-474	IC₅₀	> 100 μM Compound: 1	Antiproliferative activity against human BT474 cells after 48 hrs by Alamar blue assay Antiproliferative activity against human BT474 cells after 48 hrs by Alamar blue assay	[PMID: 28838692]
HEK293	EC₅₀	0.0937 μM Compound: FSK	Agonist activity at recombinant human AC8 expressed in human HEK293 cells assessed as fold increase in cAMP level by LANCE Ultra cAMP Detection kit method Agonist activity at recombinant human AC8 expressed in human HEK293 cells assessed as fold increase in cAMP level by LANCE Ultra cAMP Detection kit method	[PMID: 31776060]
HepG2	EC₅₀	2.7 μM Compound: Colforsin	Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis	[PMID: 20966043]
HepG2	EC₅₀	7.1 μM Compound: Colforsin	Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis	[PMID: 20966043]
HepG2	EC₅₀	7.9 μM Compound: Colforsin	Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis	[PMID: 20966043]
Hepatocyte	EC₅₀	0.7 μM Compound: Colforsin	Activation of PXR in human cryopreserved hepatocytes assessed as induction of CYP3A4 Activation of PXR in human cryopreserved hepatocytes assessed as induction of CYP3A4	[PMID: 20966043]
MCF7	IC₅₀	63.3 μM Compound: 1	Antiproliferative activity against human MCF7 cells after 48 hrs by Alamar blue assay Antiproliferative activity against human MCF7 cells after 48 hrs by Alamar blue assay	[PMID: 28838692]
NIH-3T3-G185	IC₅₀	188.2 μM Compound: Forskolin	TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	80.2 μM Compound: Forskolin	TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells	[PMID: 11716514]
Vero	CC₅₀	674 μM Compound: 10	Cytotoxicity against Vero E6 cells by MTT assay Cytotoxicity against Vero E6 cells by MTT assay	[PMID: 17663539]
Vero	EC₅₀	7.5 μM Compound: 10	Antiviral activity against SARS coronavirus in Vero E6 cells assessed as inhibition of viral replication by ELISA Antiviral activity against SARS coronavirus in Vero E6 cells assessed as inhibition of viral replication by ELISA	[PMID: 17663539]

体外研究
(In Vitro)

Forskolin (Coleonol) (GMP) 也是前列腺癌 (PC) 细胞中有效的外泌体生物合成和/或分泌激活剂^[8]。
Forskolin (GMP) 是一种从锦紫苏中分离的天然二萜 forskholii，通过其催化亚基直接激活腺苷酸环化酶 (AC)，从而增加细胞内环磷酸腺苷 (cAMP) 的水平^[1]。
Forskolin (GMP) 影响人类 T 细胞系 (如 Kit 225 和 MT-2) 的增殖。Forskolin (GMP) 处理以剂量依赖性方式抑制 Kit 225 和 MT-2 细胞的增殖，IC₅₀ 等于 ~5 μM Forskolin (GMP)。Forskolin (GMP) 处理 (10-100 μM) 将 cAMPi 水平提高到基础水平的 5 到 20 倍，达到最大水平 50-100 μM Forskolin^[6]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Forskolin (Coleonol) (GMP) 处理的 Mrp4^-/- 小鼠显示 Ki67 阳性和裂解半胱天冬酶 3 阳性 EC 数量增加，周细胞覆盖量显著减少。在从 P7 到 P12 暴露于高氧 (75% 氧气) 的幼崽中，Mrp4^-/- 小鼠显示无血管化视网膜区域显著增加^[2]。
健康大鼠组平均血糖为 102.12 mg/dL，对照组为 101.25，Forskolin (GMP) 组为 103。数据显示，Forskolin (GMP) 组在研究结束时的血糖水平较低，根据所应用的统计检验具有显著差异^[7]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

410.50

Formula

C₂₂H₃₄O₇

CAS 号

66575-29-9

中文名称

毛喉素 (GMP)

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料

产品使用指南 (1538 KB)

参考文献

[1]. Robbins JD, et al. Forskolin carbamates: binding and activation studies with type I adenylyl cyclase. J Med Chem. 1996 Jul 5;39(14):2745-52. [Content Brief]

[2]. Matsumiya W, et al. Forskolin modifies retinal vascular development in Mrp4-knockout mice. Invest Ophthalmol Vis Sci. 2012 Dec 7;53(13):8029-35. [Content Brief]

[3]. Mayati A, et al. Functional polarization of human hepatoma HepaRG cells in response to forskolin. Sci Rep. 2018 Oct 31;8(1):16115. [Content Brief]

[4]. Awad JA, et al. Interactions of forskolin and adenylate cyclase. Effects on substrate kinetics and protection against inactivation by heat and N-ethylmaleimide. J Biol Chem. 1983 Mar 10;258(5):2960-5. [Content Brief]

[5]. Seamon KB, et al. Structure-activity relationships for activation of adenylate cyclase by the diterpene forskolin and its derivatives. J Med Chem. 1983 Mar;26(3):436-9. [Content Brief]

[6]. Ríos-Silva M, et al. Effect of chronic administration of forskolin on glycemia and oxidative stress in rats with and without experimental diabetes. Int J Med Sci. 2014 Mar 11;11(5):448-52. [Content Brief]

[7]. Rodriguez G, et al. Forskolin-inducible cAMP pathway negatively regulates T-cell proliferation by uncoupling the interleukin-2 receptor complex. J Biol Chem. 2013 Mar 8;288(10):7137-46. [Content Brief]

[8]. Amrita Datta, et al. High-throughput screening identified selective inhibitors of exosome biogenesis and secretion: A drug repurposing strategy for advanced cancer. Sci Rep. 2018 May 25;8(1):8161. [Content Brief]

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质量		浓度		体积		分子量 *
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The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)	×	体积 _(start)	=	浓度 _(final)	×	体积 _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Forskolin (Synonyms: 毛喉素; Coleonol; Colforsin; HL 362)

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Forskolin (Synonyms: 毛喉素; Coleonol; Colforsin; HL 362)

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Forskolin 相关分类

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