| 货号 | 16425-25mg |
| 描述 | Acyl-CoA:diacylglycerol acyltransferase-1 (DGAT-1) catalyzes the final committed step in the biosynthesis of triglycerides and has potential roles in obesity, diabetes, and atherosclerosis.1,2,3 PF-04620110 is a potent inhibitor of DGAT-1 (IC50 = 19 nM) that is without effect on DGAT-2.4 It has high oral bioavailability (100%) in rats, with a moderate half-life of 6.8 hours.4 PF-04620110 significantly blocks an increase in plasma triglyceride levels following a corn oil bolus in rats.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Shi, Y. and Burn, P. Lipid metabolic enzymes: Emerging drug targets for the treatment of obesity. Nature Reviews.Drug Discovery 3, 695-710 (2004). 2.Zhao, G.,Souers, A.J.,Voorbach, M., et al. Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor. Journal of Medicinal Chemistry 51, 380-383 (2008). 3.Rudel, L.L.,Lee, R.G. and Cockman, T.L. Acyl coenzyme A: Cholesterol acyltransferase types 1 and 2: structure and function in atherosclerosis. Current Opinion in Lipidology 12, 121-127 (2001). 4.Dow, R.L.,Li, J.C.,Pence, M.P., et al. Discovery of PF-04620110, a potent, selective, and orally bioavailable inhibitor of DGAT-1. ACS Med.Chem.Lett. 2(5), 407-412 (2011). | |
| 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 | 396.4 |
| 分子式 | C21H24N4O4 |
| CAS号 | 1109276-89-2 |
| 稳定性 | ≥ 2 years |
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