MI-883

MI-883 is the orally active agonist for Constitutive Androstane Receptor (CAR, EC50=73 nM) and the antagonist for Pregnane X Receptor (PXR, IC50=0.1 μM) . MI-883 stimulates CAR LBD assembly (EC50=0.38 µM) and CAR3 variant activation (EC50=0.074 µM), induces CYP2B6 mRNA expression in HepaRG and primary human hepatocytes. MI-883 inhibits basal PXR activity IC50=2.03 µM) in transiently transfected HepG2 cells, blocks CYP3A4 mRNA expression in HepG2. MI-883 regulates cholesterol metabolism and bile acid excretion, improves hypercholesterolemia in mouse models[1].

Product Specifications

CAS Number

[2530027-71-3]

UNSPSC

12352005

Target

Constitutive Androstane Receptor; Cytochrome P450; Pregnane X Receptor (PXR)

Related Pathways

Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease

Smiles

O=C(C1=CC(CN2N=NC(C3=C(C4=CC=C(Cl)C=C4)N=C5C=C(C=CN53)F)=C2)=CC=C1Cl)N

Molecular Formula

C23H15Cl2FN6O

Molecular Weight

481.31

References & Citations

[1]Dusek J, et al. The hypolipidemic effect of MI-883, the combined CAR agonist/PXR antagonist, in diet-induced hypercholesterolemia model[J]. Nature Communications, 2025, 16 (1) : 1418.