Forskolin 是一种有效的腺苷酸环化酶激活剂，对 I 型腺苷酸环化酶 [1] 的 IC50 为 41 nM。 Forskolin，EC50 为 0.5 μM，也是细胞内 cAMP 形成的诱导剂 [2] Forskolin 诱导多种细胞分化，激活黄体酮 X 受体 (PXR) 和 FXR[3] Forskolin 具有对心脏有收缩作用，并具有抗血小板聚集和降压作用毛喉素还诱导自噬[4][5]。

毛喉素 (Coleonol) 也是前列腺癌 (PC) 细胞中有效的外泌体生物发生和/或分泌激活剂[7]。毛喉素对人红细胞膜自由基应激的调控及其治疗心血管疾病和糖尿病的前景[8]。毛喉素通过增加cAMP减弱细胞毒性和细胞凋亡。

体内研究表明，毛喉素主要降低健康大鼠的基础葡萄糖，并减轻糖尿病大鼠的高血糖症的严重程度[6]。 Mrp4(-/-) 小鼠在视网膜血管发育方面没有表现出明显的异常，但 Mrp4(-/-) 小鼠的视网膜血管发育在毛喉素给药后受到抑制。经毛喉素处理的 Mrp4(-/- ) 小鼠显示 Ki67 阳性和裂解半胱天冬酶 3 阳性 EC 数量增加，周细胞覆盖量显着减少，空袖数量减少[2]。

产品性质：

Cas No.：66575-29-9

别名：毛喉素; Coleonol; Colforsin

化学名： [(3R,4aR,5S,6S,6aS,10S,10aR,10bS)-3-ethenyl-6,10,10b-trihydroxy-3,4a,7,7,10a-pentamethyl-1-oxo-5,6,6a,8,9,10-hexahydro-2H-benzo[f]chromen-5-yl] acetate

Canonical SMILES CC(=O)OC1C(C2C(CCC(C2(C3(C1(OC(CC3=O)(C)C=C)C)O)C)O)(C)C)O

分子式：C22H34O7

分子量：410.5

溶解度：≥ 20.525mg/mL in DMSO

储存条件：-20°C, protect from light

注意事项：

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References:

[1]: Robbins JD, Boring DL, et,al. Forskolin carbamates: binding and activation studies with type I adenylyl cyclase. J Med Chem. 1996 Jul 5;39(14):2745-52. doi: 10.1021/jm960191+. PMID: 8709105.

[2]: Matsumiya W, Kusuhara S, et,al. Forskolin modifies retinal vascular development in Mrp4-knockout mice. Invest Ophthalmol Vis Sci. 2012 Dec 7;53(13):8029-35. doi: 10.1167/iovs.12-10781. PMID: 23154460; PMCID: PMC3517270.

[3]: Mayati A, Moreau A, et,al. Functional polarization of human hepatoma HepaRG cells in response to forskolin. Sci Rep. 2018 Oct 31;8(1):16115. doi: 10.1038/s41598-018-34421-8. PMID: 30382126; PMCID: PMC6208432.

[4]: Awad JA, Johnson RA, 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. PMID: 6681815.

[5]: Seamon KB, Daly JW, 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. doi: 10.1021/jm00357a021. PMID: 6681845.

[6]: Ríos-Silva M, Trujillo X, 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. doi: 10.7150/ijms.8034. PMID: 24688307; PMCID: PMC3970096.

[7]: Datta A, Kim H, 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. doi: 10.1038/s41598-018-26411-7. PMID: 29802284; PMCID: PMC5970137.

[8]:Niaz MA, Singh RB. Modulation of free radical stress in human red blood cell membrane by forskolin and the prospects for treatment of cardiovascular disease and diabetes. Cell Mol Biol (Noisy-le-grand). 1999 Dec;45(8):1203-7. PMID: 10643969.