CINPA1

产品名称：

102636-74-8
CINPA1
[5-[(Diethylamino)acetyl]-10,11-dihydro-5H-dibenz[b,f]azepin-3-yl]carbamic acid ethyl ester
CAR Inhibitor not PXR Activator 1
Ethyl 5-(2-(diethylamino)acetyl)-10,11-dihydro-5H-dibenzo[b,f]azepin-3-ylcarbamate

产品介绍：

产品说明

生化/生理作用

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 μM CINPA1 against 0.1 μM 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 μM CINPA1 against 5 μM rifampicin; HepG2-PXR reporter cells) and no cytotoxicity or agonist/antagonist activity toward FXR, GR, LXRα/β, PPARγ, RXRα/β, VDR.

基本信息

经验(实验)分子式	C₂₃H₂₉N₃O₃
分子量	395.49
MDL编号	MFCD00288296

产品性质

测定	≥98%
形式	powder
颜色	white to beige
溶解性	DMSO: 2 mg/mL, clear
储存温度	−20℃
SMILES string	O=C(CN(CC)CC)N1C2=C(C=CC=C2)CCC3=C1C=C(NC(OCC)=O)C=C3

安全信息

储存分类代码	13 - Non Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable