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197576-78-6

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197576-78-6

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CAS No. 197576-78-6

分子式 C22H22N2O

分子量 330.42

英文名称 RPR107393 free base

中文同义词化合物 T12765

基本信息

产品名称

197576-78-6

中文同义词

化合物 T12765

英文名称

RPR107393 free base

英文同义词

RPR107393 free base;1-Azabicyclo[2.2.2]octan-3-ol, 3-[4-(6-quinolinyl)phenyl]-

CAS No.

197576-78-6

分子式

C22H22N2O

分子量

330.42

EINECS号

MDL NO.

MFCD30533342

MOL

197576-78-6.mol

性质

密度

1.28±0.1 g/cm3(Predicted)

沸点

523.5±50.0 °C(Predicted)

酸度系数(pKa)

13.75±0.20(Predicted)

用途

靶点

IC50: 0.8±0.2 nM (rat liver microsomal squalene synthase)

体内研究

One hour after RPR107393 (10 mg/kg p.o.), Cholesterol biosynthesis is reduced by 92% with an approximate ED 50 value of 5 mg/kg. Six hours after RPR107393 (10 mg/kg p.o.) administration, Cholesterol biosynthesis is reduced by 74% (the time for 50% inhibition is ~7 hr). An 82% inhibition of hepatic Cholesterol biosynthesis is observed 10 hr after RPR107393 (25 mg/kg p.o.), but the effect is no longer apparent at 21 hr. Inhibition of Cholesterol biosynthesis by Zaragozic acid or RPR107393 is associated with an accumulation of radiolabeled diacid products in the liver. RPR107393 is a potent Cholesterol-lowering agent in rats. RPR107393 (30 mg/kg p.o. b.i.d.) lowers serum Cholesterol by 35% after 2 days and by nearly 50% after 3 days of treatment.

体外研究

RPR107393 is a selective squalene synthase inhibitor with subnanomolar potency. RPR107393 inhibits rat liver microsomal squalene synthase with an IC 50 value of 0.8±0.2 nM (n=4). In the time-course study, cells are treated with ER-27856 (1 μM), RPR-107393 (10 μM), Atorvastatin (1 μM), or NB-598 (1 μM) for 2-24 h, and lipid biosynthesis during the last 2 h of the incubation is determined. RPR-107393 (10 μM) inhibits Cholesterol biosynthesis and reduces triglyceride biosynthesis. Similarly, 1 μM RPR-107393 inhibits Cholesterol and triglyceride biosynthesis by 82.4% and 70.0%, respectively.

生物活性

RPR107393 free base 是一种有效的选择性角鲨烯合酶 (squalene synthase) 抑制剂，抑制鼠肝微粒体角鲨烯合成酶，IC50值为 0.8 nM。

编辑结构

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