133825-80-6
中文名称
N-(2,6-bis(isopropyl)phenyl)-N'-((1-(4-(dimethylaminomethyl)phenyl)cyclopentyl)methyl)urea
英文名称
N-(2,6-bis(isopropyl)phenyl)-N'-((1-(4-(dimethylaminomethyl)phenyl)cyclopentyl)methyl)urea
CAS
133825-80-6
分子式
C27H39N3O
分子量
421.62
MOL 文件
133825-80-6.mol
133825-80-6 结构式
基本信息
中文别名
化合物 T12225化合物 NEVANIMIBE
1-(2,6-二异丙基苯基)-3-((1-(4-二甲胺基)苯基)环戊基)甲基)脲
英文别名
ATR-101PD-132301
ATR 101
ATR101
PD-132301
1-(2,6-Diisopropylphenyl)-3-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea
N-(2,6-bis(isopropyl)phenyl)-N'-((1-(4-(dimethylaminomethyl)phenyl)cyclopentyl)methyl)urea
Urea, N-[2,6-bis(1-methylethyl)phenyl]-N'-[[1-[4-(dimethylamino)phenyl]cyclopentyl]methyl]-
物理化学性质
沸点528.1±50.0 °C(Predicted)
密度1.062±0.06 g/cm3(Predicted)
储存条件Sealed in dry,2-8°C
酸度系数(pKa)13.91±0.46(Predicted)
常见问题列表
生物活性
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。靶点
|
ACAT1 9 nM (EC 50 ) |
ACAT2 368 nM (EC 50 ) |
体外研究
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. |