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
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Frequently Asked Questions
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