MI-883

• CAS Number :

  2530027-71-3

• Target :

  Cytochromes P450

• Related Pathways :

  Metabolism

• Bioactivity :

  MI-883 is an orally active Constitutive Androstane Receptor (CAR, EC50=73 nM) agonist and a Pregnane X Receptor (PXR, IC50=0.1 ?M) 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.

• Smiles :

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

• Molecular Formula :

  C23H15Cl2FN6O

• Molecular Weight :

  481.309

• Shipping Conditions :

  Cool pack

• Storage Temperature :

  -20°C