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CAS No.: 166518-60-1

Avasimibe/阿伐麦布 Catalog No. CSN10357

Synonyms: CI-1011;PD-148515;Cl-1011

Avasimibe is an ACAT inhibitor with IC50 of 3.3 μM, it also inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with IC50 of 2.9/13.9 and 26.5 μM, respectively.

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生物活性

实验方案

技术信息

生物活性

描述Acyl-CoA:cholesterol acyltransferases (ACAT) are intracellular enzymes that catalyze the synthesis of cholesterol esters. Avasimibe is an inhibitor for both ACAT1 and ACAT2 with IC50 values of 24 and 9.2 μM, respectively^[3]. In human hepatic microsomes, avasimibe inhibits the activity of three human P450 isoenzymes, CYP2C9, CYP2C19, and CYP1A, with IC50 values of 2.88 ± 0.14, 26.5 ± 2.8, and 13.9 ± 5.0 μM, respectively. Avasimibe between 0.05 and 10 μM dose-dependently induced CY2C9 activity in primary cultures of human hepatocytes. For CYP2B6, avasimibe from 0.5 to 10 μM increased the enzyme activity at a concentration-dependent manner^[4]. Incubation of THP-1 cells with 0.2 μM avasimibe during the process of lipid loading for 48 hours resulted in the 70% reduction of cellular cholesteryl ester content. In HepG2 cells administered with 10 nM to 10 μM avasimibe for 24 h, the secretion of apo B 100 was dose-dependently decreased. An overnight incubation with 10 μM avasimibe also suppressed the synthesis of apo B in HepG2 cells. For apo E*3-Leiden mice, the supplementation of avasimibe (0.01%, » a daily dose of 10 mg/kg) in the diet decreased the plasma total cholesterol concentration by 56% compared to mice fed with high fat/high cholesterol diet alone.
作用机制Avasimibe is an oral inhibitor for ACAT that suppresses lipid accumulation in macrophages, thereby impeding the development of atherosclerotic lesions^[5].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
HepG2 cells	-	Function assay	-	Inhibition of ACAT in human HepG2 cells, IC50=0.479 μM	19167888
rat macrophages	-	Function assay	24 h	Inhibition of ACAT in rat macrophages assessed as incorporation of extracellular [3H]-oleic acid-BSA complex into the intracellular cholesteryl ester after 24 hrs, IC50=0.479 μM	19464189
THP1 cells	-	Function assay	-	Inhibition of ACAT-mediated esterified cholesterol accumulation in human THP1 cells exposed to acetyl-LDL during differentiation assessed as effect on foam cell formation, IC50=1.5 μM	18620381

动物研究
剂量
Mice: 7.5 mg/kg^[3] (i.v.); 15 mg/kg, 100 mg/kg^[3] (p.o.); 15 mg/kg ^[4] (i.p.) Rats: 25 mg/kg^[5]

给药途径
i.v., p.o., i.p.

动物研究
剂量	Mice: 7.5 mg/kg^[3] (i.v.); 15 mg/kg, 100 mg/kg^[3] (p.o.); 15 mg/kg ^[4] (i.p.) Rats: 25 mg/kg^[5]
给药途径	i.v., p.o., i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9931 mL
- 9.9657 mL
- 19.9314 mL
- 5 mM
- 0.3986 mL
- 1.9931 mL
- 3.9863 mL
- 10 mM
- 0.1993 mL
- 0.9966 mL
- 1.9931 mL

技术信息

CAS号

166518-60-1

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H43NO4S

运输

蓝冰

分子量

501.72

别名

CI-1011;PD-148515;Cl-1011

溶解度

DMSO	110.0 mg/mL (219.2 mM)
Water	insoluble

动物实验配方

2% DMSO+corn oil

5 mg/mL

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