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CINPA1
产品别名
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
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C23H29N3O3 |
| Molecular weight | 395.49 |
| MDL number | MFCD00288296 |
| Biochem/physiol Actions【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. |
产品性质
| Assay【测定】 | ≥98% |
| form【形式】 | powder |
| color【颜色】 | white to beige |
| solubility【溶解性】 | DMSO: 2 mg/mL, clear |
| storage temp.【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
| Storage Class Code【储存分类代码】 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
