CAR agonist 39

Chemical Structure : CAR agonist 39

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货号: PC-23985Not For Human Use, Lab Use Only.

CAR agonist 39 is a potent, selective nuclear constitutive androstane receptor (CAR, NR1I3) agonist with EC50 of 611 nM in TR-FRET assays and EC50 of 1.22 uM in CAR LBD assembly assays.

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生物&药学活性

CAR agonist 39 is a potent, selective nuclear constitutive androstane receptor (CAR, NR1I3) agonist with EC50 of 611 nM in TR-FRET assays and EC50 of 1.22 uM in CAR LBD assembly assays.
CAR agonist 39 shows no activity to activate PXR at 10 μM.
CAR agonist 39 (1 uM) could significantly upregulate CYP2B6 mRNA in primary human hepatocyte models, significantly decreases the number of cells with specific cytoplasm EGFP-hCAR + Ala localization.
CAR agonist 39 is a active ligand for all CAR variants, displays significant activity in the induction experiments in PHH and HepaRG cells irrespective of their lower affinities to wtCAR or CAR3 variants in CAR TR-FRET and cellular assays.
CAR agonist 39 regulates CAR target genes in humanized CAR mice as well as human hepatocytes, it does not activate other nuclear receptors and is nontoxic in cellular and genotoxic assays as well as in rodent toxicity studies.

物理化学性质&存储条件

分子量	463.32
分子式	C23H16Cl2N6O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-Chloro-5-((4-(2-(4-chlorophenyl)imidazo[1,2-a]pyridin-3-yl)-1H-1,2,3-triazol-1-yl)methyl)benzamide

参考文献

1. Ivana Mejdrová, et al. J Med Chem. 2023 Feb 23;66(4):2422-2456.

CAR agonist 39

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CAR agonist 39

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