The liver X receptors (LXRs) are nuclear receptors that act as ligand-dependent transcription factors. They modulate lipid, cholesterol, and carbohydrate metabolism and homeostasis. SR9238 is an inverse agonist of the two LXR isoforms, LXRα and LXRβ (IC50s = 214 and 43 nM, respectively). It displays liver specificity in vivo, with little action at peripheral LXR. SR9238 suppresses hepatic lipogenesis, inflammation, lipid accumulation, and fibrosis in mouse models of non-alcoholic steatohepatitis. It also reduces plasma cholesterol levels in diet-induced obese mice.
