11beta-Hydroxyprogesterone (11β-Hydroxyprogesterone) (Synonyms: 21-Deoxycorticosterone, 11β-OHP, 11β-hydroxy Progesterone, NSC 15469, U-1701) |
| Katalog-Nr.GC34016 |
11beta-Hydroxyprogesteron (11β-Hydroxyprogesteron) ist ein starker Inhibitor von 11&7#946;-Hydroxysteroiddehydrogenase; aktiviert auch den menschlichen Mineralokortikoidrezeptor in COS-7-Zellen mit einer ED50 von 10 nM.
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Cas No.: 600-57-7
Sample solution is provided at 25 µL, 10mM.
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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.
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