149281-19-6

中文名称 149281-19-6

英文名称 CGP-53153

CAS 149281-19-6

分子式 C23H33N3O2

分子量 383.53

MOL 文件 149281-19-6.mol

149281-19-6 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

化合物 T10780

英文别名

CGP-53153
1H-Indeno[5,4-f]quinoline-7-carboxamide, N-(1-cyano-1-methylethyl)-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-4a,6a-dimethyl-2-oxo-, (4aR,4bS,6aS,7S,9aS,9bS,11aR)-

物理化学性质

沸点627.0±55.0 °C(Predicted)

密度1.118±0.06 g/cm3(Predicted)

储存条件-20°C储存

溶解度溶于二甲基亚砜

酸度系数(pKa)12.88±0.60(Predicted)

常见问题列表

生物活性

CGP-53153是甾体类的 5 alpha reductase 抑制剂，在大鼠和人前列腺组织中的 IC50 值分别为36 nM。

靶点

IC50: 36 nM (rat 5 alpha reductase), 262 nM (human 5 alpha reductase)

体外研究

CGP-53153 competitively inhibits rat microsomal 5 alpha reductase from prostate with an IC ₅₀ of 36 nM compared to the reference compound finasteride (IC ₅₀ =11 nM). CGP 53153 is approximately one order of magnitude more potent in inhibiting rat compared to human 5 alpha reductase, with IC ₅₀ values of 36 and 262 nM, respectively

体内研究

CGP-53153 can significantly reduce T-propionate-mediated prostate growth at oral doses of 0.01 mg/kg. CGP-53153 significantly reduces prostate weight at 3 and 10 mg/kg by 31% and 37%, respectively. Treatment for 12 weeks with both CGP-53153 reduces prostate volume by more than 70% in individual dogs. Neither body weight nor the weight of any organ tested is affected by CGP-53153.