2. Signaling Pathways
  3. Vitamin D Related/Nuclear Receptor
  4. Constitutive Androstane Receptor
  5. Constitutive Androstane Receptor Agonist

Constitutive Androstane Receptor Agonist

Constitutive Androstane Receptor Agonists (2):

Cat. No. Product Name Effect Purity
  • HY-155295
    Z-CITCO
    		Agonist
    Z-CITCO is the cis isomer of CITCO (HY-103244). Z-CITCO is an agonist of constitutive androstane receptor (CAR) with an EC50 value of 3.9 µM.
  • HY-173033
    MI-883
    		Agonist
    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.