5α-Tetrahydrocorticosterone

5α-Tetrahydrocorticosterone (5α-HB), an endogenous steroid, is a glucocorticoid receptor (GR) agonist and a metabolite of Corticosterone (HY-B1618). 5α-Tetrahydrocorticosterone is an effective topical anti-inflammatory agent in vivo. 5α-Tetrahydrocorticosterone reduces metabolites that bind to GR-Corticosterone and its 5α-reduced metabolites in rat hepatocytes, with a K_d of 268 nM. 5α-Tetrahydrocorticosterone can be used for research on inflammatory skin diseases^[1]. In Vitro:5α-Tetrahydrocorticosterone (0.001-100 μM) reduces metabolites that bind to GR-Corticosterone and its 5α-reduced metabolites in rat hepatocytes, with a K_d of 268 nM^[1].
5α-Tetrahydrocorticosterone (1 μM, 16 h) increases TAT and PEPCK mRNA in H4IIE cells^[1].
5α-Tetrahydrocorticosterone (1-10000 nM, 7 days) causes concentration-dependent suppression of vessel outgrowth from mouse aortic rings, with an EC₅₀ of 2512 nM^[2].
5α-Tetrahydrocorticosterone (3 μM) increases the level of Mcp1 and Per1 and suppresses the expression of Pecam1 in aortic rings^[2].
In Vivo:5α-Tetrahydrocorticosterone (5 mg/kg, i.p., single dose) exhibits glucocorticoid effects in the mice that are bilaterally adrenalectomized^[1].
5α-Tetrahydrocorticosterone (25-200 μg, local administration, 28 days) suppresses ear swelling induced by croton-oil in the mice^[3].