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抑制劑描述：

產(chǎn)品名稱：Forskolin

產(chǎn)品別名：佛司可林;腺苷酸環(huán)化酶激活劑

英文別名：Coleonol;Colforsin

靶點：Adenylyl cyclase (AC)

CAS：66575-29-9

純度：>98 %

外觀：白色至類白色結(jié)晶粉末

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Forskolin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(zhuǎn)運蛋白和離子通道。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(chǎn)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(nèi)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(jié)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(jié)合實現(xiàn)的。Forskolin似乎對多種膜轉(zhuǎn)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。

溶解性：DMSO ：82 mg/mL (199.75 mM)

體外研究：

Forskolin increases cAMP levels in preparations of membranes, cells, or tissues. Forskolin not only activates AC but also interacts with certain other proteins, including glucose transporters and ion channels. Forskolin is able to promote activation of nine different transmembrane iso-forms of AC, albeit with somewhat less efficacy for AC9, which could be used to provides a means to identify and quantify high-affinity binding sites, i.e., G-proteins (Gs)–AC complexes. Activation of s by GPCRs contributes to Forskolin-stimulated cAMP generation in cells because of s-Forskolin potentiation of AC activity. Forskolin stimulates adenylate cyclase activity without interacting with cell surface receptors. Forskolin's potentiation of cAMP in turn inhibits basophil and mast cell degranulation and histamine release, lowers blood pressure and intraocular pressure, inhibits platelet aggregation, promotes vasodilation, bronchodilation, and thyroid hormone secretion, and stimulates lipolysis in fat cells. Forskolin inhibits the binding of platelet-activating factor (PAF), independently of cAMP formation, which may be a result of Forskolin's direct effect on PAF or via interference with PAF binding to receptor sites. Forskolin also appears to have an effect on several membrane transport proteins, and inhibits glucose transport in erythrocytes, adipocytes, platelets, and other cells. Forskolin is used to treat with glaucoma.

體內(nèi)研究：The Forskolin (Fsk)-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. The average blood glucose in the healthy rat group is 102.12±1.94 mg/dL, 101.25±3.56 for control group and 103±2.08 in forskolin group. The data shows that glucose levels at the end of the study are lower in forskolin group, with a significant difference according to the statistical tests applied (p=0.03).

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