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].
References:
- [1]. Yang H, et al. Signaling control of the constitutive androstane receptor (CAR). Protein Cell. 2014 Feb;5(2):113-23. [Content Brief]
- [2]. Molnár F, et al. An update on the constitutive androstane receptor (CAR). Drug Metabol Drug Interact. 2013;28(2):79-93. [Content Brief]
- [3]. Yan J, et al. Deciphering the roles of the constitutive androstane receptor in energy metabolism. Acta Pharmacol Sin. 2015 Jan;36(1):62-70. [Content Brief]
- [4]. Gao J, et al. The constitutive androstane receptor is an anti-obesity nuclear receptor that improves insulin sensitivity. J Biol Chem. 2009 Sep 18;284(38):25984-92. [Content Brief]
- [5]. Moore LB, et al. Orphan nuclear receptors constitutive androstane receptor and pregnane X receptor share xenobiotic and steroid ligands. J Biol Chem. 2000 May 19;275(20):15122-7. [Content Brief]
- [6]. Goodwin B, et al. Transcriptional regulation of the human CYP3A4 gene by the constitutive androstane receptor. Mol Pharmacol. 2002 Aug;62(2):359-65. [Content Brief]
All Product Categories
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Constitutive Androstane Receptor Related Products (16)
Related Products (16)
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Fluopyram
0 ImagesFluopyram is an orally active succinate dehydrogenase inhibitor, antifungal and nematicide. Fluopyram inhibits succinate dehydrogenase activity, activates CAR/PXR nuclear receptors, and increases caspase-3, TNF-α and NF-κB. Fluopyram inhibits the growth of F. virguliforme, Botrytis cinerea and Alternaria solani with EC50 values of 3.35, 5.389 and 0.244 µg/mL, respectively. Fluopyram induces liver and thyroid tumor formation. Fluopyram is nephrotoxic and embryotoxic.
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CINPA1
0 ImagesCINPA1 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.
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MI-883
0 ImagesMI-883 is orally active constitutive androstane receptor (CAR) (EC50 of 73 nM) agonist and pregnane X Receptor (PXR) (IC50 of 100 nM) antagonist. MI-883 binds to CAR and PXR ligand-binding domains, promotes CAR LBD assembly, activates CAR3 variant, stimulates CAR cytoplasmic-nuclear translocation, upregulates CAR target genes, recruits coactivators NCOA1, NCOA2, NCOA3, inhibits basal and agonist-induced PXR activation, downregulates PXR target genes, disrupts PXR-NCOR2 interaction, blocks agonist-mediated PXR-NCOA1 recruitment. MI-883 reduces plasma total cholesterol, LDL cholesterol, and hepatic free cholesterol levels, increases fecal bile acid excretion, regulates genes involved in xenobiotic metabolism, cholesterol homeostasis, and bile acid homeostasis. MI-883 exhibits metabolic stability, liver-predominant distribution, a safety profile with no observed toxicity, and does not stimulate human hepatocyte hypertrophy or hyperplasia. MI-883 can be used for the research of diet-induced hypercholesterolemia.
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Epsilon-momfluorothrin
0 ImagesEpsilon-momfluorothrin is a type I synthetic pyrethroid insecticide, activates constitutive androstane receptor (CAR), and induces hepatocellular tumors in rats.
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CT-1119
0 ImagesCat. No.: HY-P992338CT-1119 is an autologous human anti-Mesothelin chimeric antigen receptor macrophage (CAR-M). CT-1119 mediates CAR-dependent, antigen-dependent functional activities. CT-1119 acts as a phagocytosis inducer, tumor cell killer, pro-inflammatory cytokine inducer, and M1 macrophage polarizer. CT-1119 exhibits stronger resistance to M2 repolarization and reduces tumor burden in a mouse lung cancer xenograft model. CT-1119 can be used for the research of mesothelin-expressing solid tumors.
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Fluopyram (Standard)
0 ImagesFluopyram (Standard) is the analytical standard of Fluopyram (HY-119459). This product is intended for research and analytical applications. Fluopyram is an orally active succinate dehydrogenase inhibitor, antifungal and nematicide. Fluopyram inhibits succinate dehydrogenase activity, activates CAR/PXR nuclear receptors, and increases caspase-3, TNF-α and NF-κB. Fluopyram inhibits the growth of F. virguliforme, Botrytis cinerea and Alternaria solani with EC50 values of 3.35, 5.389 and 0.244 µg/mL, respectively. Fluopyram induces liver and thyroid tumor formation. Fluopyram is nephrotoxic and embryotoxic.
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Z-CITCO
0 ImagesCat. No.: HY-155295CAS No.: 2583138-04-7Z-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.
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Isobutylparaben (Standard)
0 ImagesSynonyms: Isobutyl-P-Hydroxybenzoate (Standard)Isobutylparaben (Standard) is the analytical standard of Isobutylparaben. This product is intended for research and analytical applications. Isobutylparaben (Isobutyl 4-hydroxybenzoate) is the agonist for PXR, CAR and PPAR. Isobutylparaben has a broad-spectrum antimicrobial activity and widely used in personal care products and cosmetics.
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DL5050
0 ImagesCat. No.: HY-134522CAS No.: 2259710-64-8DL5050 is a selective and potent human constitutive androstane receptor (hCAR) agonist that does not activate pregnane X receptor (PXR). DL5050 preferentially induces the expression of CYP2B6 (target of hCAR) over CYP3A4 (target of hPXR) on both the mRNA and protein levels. DL5050 can be used for the researches of cancer and metabolic disease, such as diabetes.
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Isobutylparaben-d4
0 ImagesSynonyms: Isobutyl 4-hydroxybenzoate-d4Isobutylparaben-d4 is the deuterium labeled Isobutylparaben. Isobutylparaben (Isobutyl 4-hydroxybenzoate) is the agonist for PXR, CAR and PPAR. Isobutylparaben has a broad-spectrum antimicrobial activity and widely used in personal care products and cosmetics.
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S07662
0 ImagesCat. No.: HY-110134CAS No.: 883226-64-0S07662 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).
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Panaxytriol
0 ImagesCat. No.: HY-W709413CAS No.: 87005-03-6Panaxytriol is an active component of ginseng. Panaxytriol inhibits the nuclear translocation of NF-κB, thereby reducing the production of pro-inflammatory factors (such as TNF-α, IL-1β, IL-6) and nitric oxide (NO) induced by LPS (HY-D1056). Panaxytriol upregulates CYP3A4 by activating the nuclear receptor PXR/CAR. Panaxytriol improves motor dysfunction in a mouse model of brain inflammation. Panaxytriol can be used in the research of neurodegenerative diseases (such as Alzheimer's disease).
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5α-Androstan-3α-ol
0 ImagesCat. No.: HY-W722556CAS No.: 7657-50-3Synonyms: 3α,5α-Androstanol5α-Androstan-3α-ol is a γ-aminobutyric acid (GABA) receptor agonist. 5α-Androstan-3α-ol can inhibit the transcriptional activity of the orphan nuclear receptor CAR (constitutive androstane receptor). 5α-Androstan-3α-ol negatively regulates the activity of CAR by binding to CAR and promoting its dissociation from coactivator proteins. 5α-Androstan-3α-ol can be used to study nuclear receptor-mediated hormone metabolism and drug detoxification mechanisms.
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DL5055
0 ImagesCat. No.: HY-173465CAS No.: 2259710-89-7DL5055 (compound 6k) is a potent and selective hCAR activator with an EC50 of 0.35 μM. DL5055 induces CYP2B6 expression and hCAR nuclear translocation in human primary hepatocytes.
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Ethoxyquin dimer
0 ImagesEthoxyquin 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.
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