Synonyms: CAR Inhibitor not PXR Activator 1; Ethyl 5-(2-(diethylamino)acetyl)-10,11-dihydro-5H-dibenzo[b,f]azepin-3-ylcarbamate; [5-[(Diethylamino)acetyl]-10,11-dihydro-5H-dibenz[b,f]azepin-3-yl]carbamic acid ethyl ester
Molecular Formula: C23H29N3O3
Molecular Weight: 395.49
Linear Structural Formula: C23H29N3O3
MDL Number: MFCD00288296
Purity: >=98%
Storage: -20C
Biochem Physiol Actions: CINPA1 is a ligand-binding domain (LBD)-targeting constitutive androstane receptor (CAR) inhibitor that prevents CAR recruitment to promoter regions of regulated genes (by >85%; 1 muM CINPA1 against 0.1 muM CITCO-induced CAR recruitment to CYP2B6 or CYP3A4 promoters; human hepatocytes) by altering CAR-coregulator interactions. CINPA1 inhibits CAR-mediated transcription in a potent (IC50 = 70 nM; HepG2-hCAR1 CYP2B6-luc reporter cells) and selective manner with only weak PXR antagonist potency (68% inhibition by 18 muM CINPA1 against 5 muM rifampicin; HepG2-PXR reporter cells) and no cytotoxicity or agonist/antagonist activity toward FXR, GR, LXRalpha/beta, PPARgamma, RXRalpha/beta, VDR.