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102636-74-8 | CINPA1


SKU : MC502827

CAS Number : 102636-74-8

Molecular Formula : C23H29N3O3 | Molecular Weight : 395.49

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Purity NLT 98%
Storage at 20ºC 2 years

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Chemical Name CINPA1
CAS Number 102636-74-8
Molecular Formula C23H29N3O3
Molecular Weight 395.49
Introduction of 102636-74-8 :

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[1]. IC50 & Target: IC50: ~70 nM (CAR)[1] In Vitro: CINPA1 (1μM ; 24 hours) inhibits CAR-mediated transactivation without activating PXR in HepG2 cells[1].
CINPA1 is a specific xenobiotic receptor inhibitor and has no cytotoxic effects up to 30 μM[1].
CINPA1 inhibits CAR-mediated gene expression in primary human hepatocytes, where CAR is endogenously expressed[1].
CINPA1 does not alter the protein levels or subcellular localization of CAR[1].
CINPA1 increases corepressor and reduces coactivator interaction with the CAR ligand-binding domain in mammalian two-hybrid assays[1].
CINPA1 disrupts CAR binding to the promoter regions of target genes in chromatin immunoprecipitation assays[1].
CINPA1 efficiently inhibits CAR-LBD interaction with the coactivator peptide that suggesting that CINPA1 is a ligand of CAR[1].

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