Pregnenolone 16α-carbonitrile

Pregnenolone 16α-carbonitrile is a synthetic steroidal compound that acts as a prototypical and effective agonist of the rodent pregnane X receptor (PXR). It is orally active and primarily used in research to study the effects of PXR activation. PXR is a ligand-dependent nuclear receptor involved in xenobiotic metabolism, regulating drug-metabolizing enzymes and drug transporters. Pregnenolone 16α-carbonitrile also functions as a glucocorticoid receptor antagonist and has been shown to induce the expression of cytochrome P450 enzymes, particularly the CYP3A family. It is used to investigate the regulation of steroidogenesis, including testosterone biosynthesis in rodent Leydig cells, where its activation of PXR leads to down-regulation of key steroidogenic enzymes and reduced testosterone production.

Other names

Pregnenolone carbonitrile5-Pregnen-3β-ol-20-one-16α-carbonitrile