5α-Tetrahydrocorticosterone (5α-HB) is an endogenous steroid that acts as an agonist of the glucocorticoid receptor (GR) and a metabolite of corticosterone. It serves as an effective topical anti-inflammatory agent in vivo. In rat liver cells, it decreases the binding of metabolites to the glucocorticoid receptor-corticosterone and its 5α-reduced metabolites, with a Kd value of 268 nM. 5α-Tetrahydrocorticosterone is applicable in research on inflammatory skin diseases.

5α-Tetrahydrocorticosterone, at concentrations ranging from 0.001 to 100 μM, reduces the binding of metabolites to glucocorticoid receptor-corticosterone and its 5α-reduced metabolites in rat hepatocytes, with a Kd value of 268 nM. At a concentration of 1 μM for 16 hours, it enhances the expression of TAT and PEPCK mRNA in H4IIE cells. Additionally, 5α-Tetrahydrocorticosterone, when used at 1-10000 nM over 7 days, inhibits angiogenesis in mouse aortic rings in a concentration-dependent manner, with an EC50 value of 2512 nM. At 3 μM, it increases the levels of Mcp1 and Per1, while it suppresses the expression of Pecam1 in aortic rings.

5α-Tetrahydrocorticosterone (administered at 5 mg/kg via intraperitoneal injection, single dose) exhibits glucocorticoid-like effects in mice that have undergone bilateral adrenalectomy. Additionally, 5α-Tetrahydrocorticosterone (applied topically in doses of 25-200 μg over 28 days) effectively inhibits ear swelling induced by croton oil in mice.