Pricing updated 2019-07-17. Prices are subject to change without notice.
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
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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 Curr. Opin. Lipidol. 12(2), 121-127 (2001).
Dow, R.L., Li, J.C., Pence, M.P., et al. Discovery of PF-