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

Constitutive Androstane Receptor

CAR; NR1I3

Constitutive Androstane Receptor (CAR) is a nuclear receptor. The upstream targets of CAR include protein phosphatase 2A (PP2A), extracellular signal-regulated kinase (ERK), p38 mitogen-activated protein kinase (MAPK), epidermal growth factor receptor (EGFR), and various transcription factors such as hepatocyte nuclear factor 4α (HNF4α). PP2A participates in the dephosphorylation of CAR and promotes its nuclear translocation; ERK and MAPK regulate the activity of CAR by affecting its phosphorylation state; EGFR can indirectly regulate the activation of CAR; and transcription factors regulate the expression level of CAR. The downstream hot targets of CAR include many drug metabolizing enzymes and transporter genes, such as CYP2B6 and CYP3A4 in the cytochrome P450 enzyme system (CYP), as well as energy metabolism-related genes such as lipogenesis genes and gluconeogenesis-related genes. CAR activation can improve insulin sensitivity and alleviate the symptoms of obesity and type 2 diabetes; however, its abnormal activation may also be associated with the occurrence and development of liver tumors. CAR plays a key role in drug metabolism, energy metabolism, obesity, type 2 diabetes, and cancer development[1][2][3][4][5][6].

Constitutive Androstane Receptor Related Products (6):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-110249
    CINPA1
    		99.90%
    CINPA1 is a potent and specific inhibitor of constitutive androstane receptor (CAR) that does not activate pregnane X receptor (PXR). CINPA1 reduces CAR-mediated transcription with an IC50 of ~70 nM. CINPA1 can be used as a molecular tool for understanding CAR function.
    CINPA1
  • HY-111634
    Epsilon-momfluorothrin
    		99.76%
    Epsilon-momfluorothrin is a type I synthetic pyrethroid insecticide, activates constitutive androstane receptor (CAR), and induces hepatocellular tumors in rats.
    Epsilon-momfluorothrin
  • 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.
    Z-CITCO
  • HY-110134
    S07662
    		Inhibitor
    S07662 is a human constitutive androstane receptor (hCAR) inhibitor with an IC50 of 0.7 μM. S07662 recruits the corepressor NCoR in cell-based assays and attenuate the expression of CYP2B6 mRNA in human primary hepatocytes induced by phenytoin (HY-B0448) and CITCO (HY-103244).
    S07662
  • 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.
    MI-883
  • HY-138291
    Ethoxyquin dimer
    Ethoxyquin dimer is a dimer of Ethoxyquin (HY-B1425). Ethoxyquin dimer is an antioxidant. Ethoxyquin dimer can more readily accumulate in liver and adipose tissue compared with Ethoxyquin. Ethoxyquin above 10 mg/kg shows hepatotoxicity in mice.
    Ethoxyquin dimer