For research use only. Not for therapeutic Use.
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].
CINPA1 (1μM ; 24 hours) inhibits CAR-mediated transactivation without activating PXR in HepG2 cells[1].?
CINPA1 is a specific xenobiotic receptor inhibitor[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].
| Catalog Number | I011252 |
| CAS Number | 102636-74-8 |
| Synonyms | ethyl N-[11-[2-(diethylamino)acetyl]-5,6-dihydrobenzo[b][1]benzazepin-2-yl]carbamate |
| Molecular Formula | C23H29N3O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C23H29N3O3/c1-4-25(5-2)16-22(27)26-20-10-8-7-9-17(20)11-12-18-13-14-19(15-21(18)26)24-23(28)29-6-3/h7-10,13-15H,4-6,11-12,16H2,1-3H3,(H,24,28) |
| InChIKey | AYQBYSPEGRYKFA-UHFFFAOYSA-N |
| SMILES | CCN(CC)CC(=O)N1C2=CC=CC=C2CCC3=C1C=C(C=C3)NC(=O)OCC |
| Reference | [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. |
