102636-74-8

102636-74-8 structure
102636-74-8 structure
  • Name: CINPA 1
  • Chemical Name: CINPA1
  • CAS Number: 102636-74-8
  • Molecular Formula: C23H29N3O3
  • Molecular Weight: 395.49
  • Catalog: Research Areas Metabolic Disease
  • Create Date: 2020-01-23 13:46:51
  • Modify Date: 2025-08-27 10:21:52
  • 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].

Name CINPA1
Description 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].
Related Catalog
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].
References

[1]. Cherian MT, et al. CINPA1 is an inhibitor of constitutive androstane receptor that does not activate pregnane X receptor. Mol Pharmacol. 2015 May;87(5):878-89.

Molecular Formula C23H29N3O3
Molecular Weight 395.49
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