MI-883 - CAS 2530027-71-3

MI-883 is an orally active Constitutive Androstane Receptor (CAR, EC50=73 nM) agonist and a Pregnane X Receptor (PXR, IC50=0.1 μM) antagonist. It enhances CAR LBD assembly (EC50=0.38 μM) and activates the CAR3 variant (EC50=0.074 μM), inducing CYP2B6 mRNA expression in HepaRG and primary human hepatocytes. Additionally, MI-883 inhibits the basal activity of PXR (IC50=2.03 μM) and reduces CYP3A4 mRNA expression in transiently transfected HepG2 cells. It also regulates cholesterol metabolism and bile acid excretion, improving hypercholesterolemia in mouse models.

Cytochromes P450

Metabolism

2529953

C23H15Cl2FN6O

481.309

O=C(N)C1=CC(=CC=C1Cl)CN2N=NC(=C2)C3=C(N=C4C=C(F)C=CN43)C=5C=CC(Cl)=CC5

-20°C

Ice Packs

Small Compound