5α-Androstan-3β-ol is a steroidal androgen.It binds to the androgen receptor in a cell-free assay (IC50 = 1.7 µM) and activates the pregnane X receptor (PXR) in HepG2 cells in a reporter assay (EC50 = 0.8 µM). 5α-Androstan-3β-ol also inhibits the androst-4-ene-3,17-dione hydroxylase activities of 16α- and 6β-hydroxylase but not 16β- or 7α-hydroxylase (IC50s = 70, 110, >150, and >150 µM, respectively). It decreases testis weight and sperm production in mice when administered at a dose of 30 mg/kg.