133825-80-6
中文名稱
N-(2,6-bis(isopropyl)phenyl)-N'-((1-(4-(dimethylaminomethyl)phenyl)cyclopentyl)methyl)urea
英文名稱
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 結(jié)構(gòu)式
基本信息
中文別名
化合物 T12225化合物 NEVANIMIBE
1-(2,6-二異丙基苯基)-3-((1-(4-二甲胺基)苯基)環(huán)戊基)甲基)脲
英文別名
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]-
物理化學性質(zhì)
沸點528.1±50.0 °C(Predicted)
密度1.062±0.06 g/cm3(Predicted)
儲存條件Sealed in dry,2-8°C
酸度系數(shù)(pKa)13.91±0.46(Predicted)
常見問題列表
生物活性
Nevanimibe (PD-132301) 是一種口服有效的，選擇性酰基輔酶 A：膽固醇 O-?；D(zhuǎn)移酶 1 (ACAT1) 抑制劑，EC50 為 9 nM。Nevanimibe 抑制 ACAT2，EC50 為 368 nM。Nevanimibe 誘導細胞凋亡 (apoptosis)，并具有抗腎上腺皮質(zhì)癌的潛力。靶點
|
ACAT1 9 nM (EC 50 ) |
ACAT2 368 nM (EC 50 ) |
體外研究
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. |