11beta-Hydroxyprogesterone

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. IC50 & Target:ED50: 10 nM (human mineralocorticoid receptor, COS-7 cell )^[1] In Vitro: 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 mpkCCD_cl4 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]. In Vivo: 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].