DGAT-1 inhibitor | CAS:701232-20-4

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Name:T863; DGAT-1 inhibitor
Cat. No. :CS-0300
CAS No. :701232-20-4
Formula:C22H26N4O3
M. Wt. : 394.47
Solubility:10 mM in DMSO

T-863(DGAT-1 inhibitor) is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells.IC50 value:Target: DGAT1T863 causes weight loss, reduction in serum and liver triglycerides, and improved insulin sensitivity in obese mice.

Cao J, 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. Qian Y, et al. Discovery of orally active carboxylic acid derivatives of 2-phenyl-5-trifluoromethyloxazole-4-carboxamide as potent diacylglycerol acyltransferase-1 inhibitors for the potential treatment of obesity and diabetes. J Med Chem. 2011 Apr 14;54(7):2433-46. Dow RL, et al. Design and synthesis of potent, orally-active DGAT-1 inhibitors containing a dioxino[2,3-d]pyrimidine core. Bioorg Med Chem Lett. 2011 Oct 15;21(20):6122-5.