| 货号 | 16429-25mg |
| 描述 | Lipoprotein-associated phospholipase A2(Lp-PLA2), also known as platelet activating factor acetylhydrolase (PAF-AH) or phospholipase A2 group 7 (PLA2G7), hydrolyzes glycerophospholipids to produce lyso-PAF/lyso-phosphatidylcholine and short and/or oxidized fatty acids, many of which have pro-inflammatory or pro-oxidative activities.1,2 Darapladib is a reversible inhibitor of Lp-PLA2(IC50 = 0.25 nM).3 It produces sustained inhibition of plasma Lp-PLA2 activity in humans receiving intensive atorvastatin therapy.4Lp-PLA2 inhibition with darapladib also reduces the development of coronary atherosclerotic plaques.5,6 |
| 别名 | SB-480848; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Marathe, G.K.,Pandit, C.,Lakshmikanth, C.L., et al. To hydrolyse or not to hydrolyse: The dilemma of platelet activating factor acetylhydrolase (PAF-AH). Journal of Lipid Research 55(9), 1847-1854 (2014). 2.Stafforini, D.M. and Zimmerman, G. Unraveling the PAF-AH/Lp-PLA2 controversy. Journal of Lipid Research 55(9), 1811-1814 (2014). 3.Blackie, J.A.,Bloomer, J.C.,Brown, M.J., et al. The identification of clinical candidate SB-480848: A potent inhibitor of lipoprotein-associated phospholipase A2. Bioorganic & Medicinal Chemistry Letters 13(6), 1067-1070 (2003). 4.Mohler, E.R., III,Ballantyne, C.M.,Davidson, M.H., et al. The effect of darapladib on plasma lipoprotein-associated phospholipase A2 activity and cardiovascular biomarkers in patients with stable coronary heart disease or coronary heart disease risk equivalent: the results of a multicenter, randomized, double-blind, placebo-controlled study. Journal of the American College of Cardiology 51(17), 1632-1641 (2008). 5.Serruys, P.W.,García-García, H.M.,Buszman, P., et al. Effects of the direct lipoprotein-associated phospholipase A2 inhibitor darapladib on human coronary atherosclerotic plaque. Circulation 118(11), 1172-1182 (2008). 6.Wilensky, R.L.,Shi, Y.,Mohler, E.R., III, et al. Inhibition of lipoprotein-associated phospholipase A2 reduces complex coronary atherosclerotic plaque development. Nature Medicine 14(10), 1059-1066 (2008). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 666.8 |
| 分子式 | C36H38F4N4O2S |
| CAS号 | 356057-34-6 |
| 稳定性 | ≥ 2 years |
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