| 货号 | 17235-50mg |
| 描述 | Acyl-coenzyme A:cholesterol acyltransferase 1 (ACAT-1) is a sterol O-acyltransferase that catalyzes the formation of fatty acid-cholesterol esters, an important step in lipoprotein assembly and dietary cholesterol absorption.1,2 CI-976 is a potent, selective inhibitor of ACAT-1 (IC50 = 73 nM).3,4 It is orally bioavailable and decreases plasma total cholesterol, very low density lipoprotein (VLDL) cholesterol, LDL cholesterol, apolipoprotein B, liver cholesteryl esters, and VLDL and LDL cholesteryl ester content in rabbits given a diet that induces hypercholesterolemia.5 CI-976 also diminishes atherosclerotic activity in hypercholesterolemic rabbits.6 |
| 别名 | PD 128042; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Buhman, k.K.,Chen, H.C. and Farese, R.V., Jr. The enzymes of neutral lipid synthesis. The Journal of Biological Chemisty 276(44), 40369-40372 (2001). 2.Shi, Y. and Burn, P. Lipid metabolic enzymes: Emerging drug targets for the treatment of obesity. Nature Reviews.Drug Discovery 3, 695-710 (2004). 3.Field, F.J.,Albright, E. and Mathur, S. Inhibition of acylcoenzyme A: cholesterol acyltransferase activity by PD128O42: Effect on cholesterol metabolism and secretion in CaCo-2 cells. Lipids 26(1), 1-8 (1991). 4.OBrien, P.M.,Sliskovic, D.R.,Blankley, C.J., et al. Inhibitors of acyl-CoA:cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 8. Incorporation of amide or amine functionalities into a series of disubstituted ureas and carbamates. Effects on ACAT inhibition in vitro and efficacy in vivo. J.Med.Chem 37(12), 1810-1822 (1994). 5.Krause, B.R.,Pape, M.E.,Kieft, K., et al. ACAT inhibition decreases LDL cholesterol in rabbits fed a cholesterol-free diet. Arteriosclerosis and Thrombosis 14, 598-604 (1994). 6.Bocan, T.M.A.,Mueller, S.B.,Uhlendorf, P.D., et al. Comparison of CI-976, an ACAT inhibitor, and selected lipid-lowering agents for antiatherosclerotic activity in iliac-femoral and thoracic aortic lesions. Arteriosclerosis and Thrombosis 11, 1830-1843 (1991). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 393.6 |
| 分子式 | C23H39NO4 |
| CAS号 | 114289-47-3 |
| 稳定性 | ≥ 2 years |
| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |