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Avasimibe

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Chemical Structure| 166518-60-1 同义名 : CI-1011;PD-148515;Cl-1011
CAS号 : 166518-60-1
货号 : A156472
分子式 : C29H43NO4S
纯度 : 99%+
分子量 : 501.721
MDL号 : MFCD00934956
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(209.28 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

2% DMSO+corn oil 5 mg/mL

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
细胞系 浓度 检测类型 检测时间 活动说明 数据源
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
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.99mL

0.40mL

0.20mL

9.97mL

1.99mL

1.00mL

19.93mL

3.99mL

1.99mL
参考文献

[1]31(5):1108-15.

[2]110(21):3372-7.

[3]Ohshiro T, Matsuda D, Sakai K, Degirolamo C, Yagyu H, Rudel LL, Omura S, Ishibashi S, Tomoda H. Pyripyropene A, an acyl-coenzyme A:cholesterol acyltransferase 2-selective inhibitor, attenuates hypercholesterolemia and atherosclerosis in murine models of hyperlipidemia. Arterioscler Thromb Vasc Biol. 2011 May;31(5):1108-15.