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浙江省杭州市萧山区宁围街道传化科创大厦2幢6层

Forskolin

目录号
C665752
产品规格
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产品介绍

DESCRIPTION

Background

Forskolin (Coleonol) 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 is also an inducer of intracellular cAMP formation[2]. Forskolin induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR[3]. Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy[1][2][3].

Alias

毛喉素; Coleonol; Colforsin

M. W t

410.50

Formula

C22H34O7

CAS No

66575-29-9

Storage

Powder

-20°C  

3 years                          

In solvent

-80°C 

6 months                                 

 

-20°C      

1 month

Solubility

DMSO

100 mg/mL(243.61 mM; Need ultrasonic)

 

Ethanol

82 mg/mL(199.76 mM)

 

H2O

< 0.1 mg/mL(insoluble)

 

 


技术参数

BIOLOGICAL ALTIVITY

In Vitro  

Forskolin (Fsk) is a naturally occurring diterpene isolated from Coleus forskholii, directly activates adenylyl cyclase (AC) through its catalytic subunit to increase intracellular levels of cyclic adenosine monophosphate (cAMP)[1].

Forskolin (Fsk) affects the proliferation of the human T-cell lines such as Kit 225 and MT-2. Forskolin treatment inhibits the proliferation of both Kit 225 and MT-2 cells in a dose-dependent manner with an IC50 equal to ~5 μM Fsk. Forskolin treatment (10-100 μM) increases cAMPi levels ~5- to 20-fold above basal levels, which reache maximum levels between 50-100 μM Forskolin[4].

In Vivo  

The Forskolin (Coleonol)-treated Mrp4-/- mice shows an increased number of Ki67-positive and cleaved caspase 3-positive ECs, a significant decrease in the amount of pericyte coverage, and a reduced number of empty sleeves. In pups exposed to hyperoxia (75% oxygen) from P7 to P12, the Mrp4-/- mice shows a significant increase in the unvascularized retinal area[2].

REFERENCES

[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.

[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.

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

[4]. 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.

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