Pregnenolone carbonitrile (PCN) is a catatoxic steroid that acts as an agonist of the rodent pregnane X receptor (PXR) at μM concentrations. It has been shown to mediate induction of hepatic cytochrome P450 3A, organic anion transporting peptide-2, and cholesterol 7α-hydroxylase, regulating both xenobiotic and bile acid homeostasis by enhancing hepatic uptake and biliary excretion. Activation of PXR by 50 mg/kg PCN administered to obesity-prone AKR/J mice has been reported to attenuate the development of high-fat diet-induced obesity and insulin resistance.
