N-(2,6-bis(isopropyl)phenyl)-N'-((1-(4-(dimethylaminomethyl)phenyl)cyclopentyl)methyl)urea
| 中文名称 | N-(2,6-bis(isopropyl)phenyl)-N'-((1-(4-(dimethylaminomethyl)phenyl)cyclopentyl)methyl)urea |
|---|---|
| 中文同义词 | 1-(2,6-二异丙基苯基)-3-((1-(4-二甲胺基)苯基)环戊基)甲基)脲;化合物 T12225 |
| 英文名称 | N-(2,6-bis(isopropyl)phenyl)-N'-((1-(4-(dimethylaminomethyl)phenyl)cyclopentyl)methyl)urea |
| 英文同义词 | N-(2,6-bis(isopropyl)phenyl)-N'-((1-(4-(dimethylaminomethyl)phenyl)cyclopentyl)methyl)urea;ATR-101;1-(2,6-Diisopropylphenyl)-3-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea;Urea, N-[2,6-bis(1-methylethyl)phenyl]-N'-[[1-[4-(dimethylamino)phenyl]cyclopentyl]methyl]-;PD-132301;ATR 101; ATR101; PD-132301 |
| CAS号 | 133825-80-6 |
| 分子式 | C27H39N3O |
| 分子量 | 421.62 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 133825-80-6.mol |
| 结构式 |  |
N-(2,6-bis(isopropyl)phenyl)-N'-((1-(4-(dimethylaminomethyl)phenyl)cyclopentyl)methyl)urea 性质
| 沸点 | 528.1±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.062±0.06 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 酸度系数(pKa) | 13.91±0.46(Predicted) |
Nevanimibe (PD-132301) 是一种口服有效的，选择性酰基辅酶 A：胆固醇 O-酰基转移酶 1 (ACAT1) 抑制剂，EC50 为 9 nM。Nevanimibe 抑制 ACAT2，EC50 为 368 nM。Nevanimibe 诱导细胞凋亡 (apoptosis)，并具有抗肾上腺皮质癌的潜力。
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ACAT1 9 nM (EC 50 ) |
ACAT2 368 nM (EC 50 ) |
Coincubation of Nevanimibe (PD-132301; ATR101; 3 nM-30 μM) and Cholesterol markedly increases toxicity in a dose-dependent manner, where 3 nM Nevanimibe in the presence of 60 μg/mL Cholesterol reduces survival by 60% after 24 hours. All doses of Nevanimibe (3 nM-30 μM) induces cytoxicity in the presence of Cholesterol, whereas treatment with Cholesterol in the absence of Nevanimibe has no effect on cell viability.
Cell Cytotoxicity Assay
| Cell Line: | The H295R and HAC clone 15 (HAC15) human ACC cell lines |
| Concentration: | 3 nM-30 μM |
| Incubation Time: | 24 hours |
| Result: | 3 nM-3 μM exhibited no toxicity, whereas 30 μM treatment reduced survival by approximately 40% within 24 hours. |