Pregnane X receptor antagonist MI-891 reduces hepatic triglycerides in PXR-CAR-CYP3A4/3A7-humanized mice.

Hepatic steatosis is a major metabolic concern associated with activation of the pregnane X receptor (PXR), a nuclear receptor known to promote lipogenesis and lipid accumulation in the liver. While the lipogenic effects of PXR agonists are well documented, there is no comprehensive data on the metabolic consequences of PXR inhibition. Here, we evaluated the impact of MI-891, a novel human PXR antagonist and inverse agonist, on hepatic lipid metabolism in high-fat diet (HFD)-fed PXR-CAR-CYP3A4/3...