11beta-Hydroxyprogesterone是11β-羟基甾类脱氢酶(11β-Hydroxysteroiddehydrogenase)的有效抑制剂;同时在COS-7细胞中激活人类盐皮质激素受体，ED50值为10nM。
CAS：600-57-7
分子式：C21H30O3
分子量：330.46
纯度：98%
存储：Store at -20°C

Background:

11beta-Hydroxyprogesterone is a potent inhibitors of 11β-Hydroxysteroid dehydrogenase; also activates human mineralocorticoid receptor in COS-7 cells with an ED50 of 10 nM.

11OHP displays agonist mineralocorticoid activity. 11β-hydroxyprogesterone activates the transiently expressed hMR in COS-7 cells in a dose-dependent manner with an ED50 of 10 nM and stimulates Ams/sc in mpkCCDcl4 cells. Docking 11β-hydroxyprogesterone within the hMR-ligand-binding domain homology model reveals that the agonist activity of 11OHP is caused by contacts between its 11β-hydroxyl group and Asn770[1].

11β-hydroxyprogesterone causes a significant elevation in blood pressure within 3 days, an effect that persisted throughout the 14-day infusion. 11β-hydroxyprogesterone is potently hypertensinogenic in the rat and that this activity depends on an intact adrenal and at least in part on the activation of mineralocorticoid receptors[2].

[1]. Rafestin-Oblin ME, et al. 11beta-hydroxyprogesterone acts as a mineralocorticoid agonist in stimulating Na+ absorption in mammalian principal cortical collecting duct cells. Mol Pharmacol. 2002 Dec;62(6):1306-13. [2]. Souness GW, et al. 11 alpha- and 11 beta-hydroxyprogesterone, potent inhibitors of 11 beta-hydroxysteroid dehydrogenase, possess hypertensinogenic activity in the rat. Hypertension. 1996 Mar;27(3 Pt 1):421-5.