942999-61-3

DGAT-1 inhibitor 2 is an effective inhibitor of DGAT-1;antiobesity agents. IC50 value: Target: DGAT-1 Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) is one of two known DGAT enzymes that catalyze the final step in triglyceride synthesis. Findings from genetically modified mice as well as pharmacological studies suggest that inhibition of DGAT1 is a promising strategy for the treatment of obesity and type 2 diabetes.

[1] Matsuda D, Tomoda H. DGAT inhibitors for obesity. Curr Opin Investig Drugs. 2007 Oct;8(10):836-41. PMID:17907060
[2] Birch, Alan M.; Birtles, Susan; Buckett, Linda K. et al. Discovery of a Potent, Selective, and Orally Efficacious Pyrimidinooxazinyl Bicyclooctaneacetic Acid Diacylglycerol Acyltransferase-1 Inhibitor. Journal of Medicinal Chemistry (2009), 52(6), 1558-15 DOI:10.1021/jm801507v
[3] King AJ, Judd AS, Souers AJ. Inhibitors of diacylglycerol acyltransferase: a review of 2008 patents. Expert Opin Ther Pat. 2010 Jan;20(1):19-29. DOI:10.1517/13543770903499305
[4] Cao J, Zhou Y, Peng H et al. Targeting Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) with small molecule inhibitors for the treatment of metabolic diseases. J Biol Chem. 2011 Dec 2;286(48):41838-51. DOI:10.1074/jbc.M111.245456