| 货号 | 18129-5mg |
| 描述 | Acyl-Coenzyme A:cholesterol acyltransferases (ACAT1 and ACAT2) catalyze the formation of cholesterol esters from cholesterol and long chain fatty acyl-coenzyme A, and may play a role in the development of atherosclerosis.1 Avasimibe is an orally bioavailable inhibitor of ACAT (IC50s = 24 and 9.2 µM for ACAT1 and ACAT2, respectively).2 It reduces foam cell formation in human macrophages in vitro, enhancing free cholesterol efflux and inhibiting the uptake of modified LDL and dose-dependently reduces plasma total triglyceride and VLDL cholesterol levels in cholesterol-fed animal models.3,4 Avasimibe inhibition of ACAT has been used to decrease amyloid β generation in models of Alzheimer’s disease.5 |
| 别名 | Cl-1011;PD-148515; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Buhman, K.F.,Accad, M. and Farese, R.V., Jr. Mammalian acyl-CoA:cholesterol acyltransferases. Biochimica et Biophysica Acta 1529, 142-154 (2000). 2.Ohshiro, T.,Matsuda, D.,Sakai, K., et al. Pyripyropene A, an acyl-coenzyme A:cholesterol acyltransferase 2-selective inhibitor, attenuates hypercholesterolemia and atherosclerosis in murine models of hyperlipidemia. Arteriosclerosis, Thrombosis, and Vascular Biology 31, 1108-1115 (2011). 3.Llaverías, G.,Laguna, J.C. and Alegret, M. Pharmacology of the ACAT inhibitor avasimibe (CI-1011). Cardiovascular Drug Reviews 21(1), 33-50 (2003). 4.Burnett, J.R.,Wilcox, L.J.,Telford, D.E., et al. Inhibition of ACAT by avasimibe decreases both VLDL and LDL apolipoprotein B production in miniature pigs. Journal of Lipid Research 40, 1317-1327 (1999). 5.Huttunen, H.J.,Peach, C.,Bhattacharyya, R., et al. Inhibition of acyl-coenzyme A: cholesterol acyl transferase modulates amyloid precursor protein trafficking in the early secretory pathway. The FASEB Journal 23(11), 3819-3828 (2009). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 501.7 |
| 分子式 | C29H43NO4S |
| CAS号 | 166518-60-1 |
| 稳定性 | ≥ 2 years |
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