dgat-1-in-1

DGAT1-IN-1 is a potent inhibitor of diacylglycerol O-acyltransferase type 1 (DGAT1) with an IC50 of less than 10 nM.

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: DGAT1 T863 (DGAT-3) causes weight loss, reduction in serum and liver triglycerides, and improved insulin sensitivity in obese mice.

Phenylpyropene A is a fungal metabolite originally isolated from P. griseofulvum that has enzyme inhibitory and insecticidal activities.1,2,3 It inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 0.8 μM).1 Phenylpyropene A inhibits diacylglycerol acyltransferase (DGAT) in rat liver microsomes (IC50 = 78.7 μM). It induces mortality in 100% of M. persicae when used at a concentration of 5 ppm.3 |1. Kwon, O.E., Rho, M.C., Song, H.Y., et al. Phenylpyropene A and B, new inhibitors of acyl-CoA: Cholesterol acyltransferase produced by Penicillium griseofulvum F1959. J. Antibiot. (Tokyo) 55(11), 1004-1008 (2002).|2. Lee, S.W., Rho, M.C., Choi, J.H., et al. Inhibition of diacylglycerol acyltransferase by phenylpyropenes produced by Penicillium griseofulvum F1959. J. Microbiol. Biotechnol. 18(11), 1785-1788 (2008).|3. Horikoshi, R., Goto, K., Mitomi, M., et al. Identification of pyripyropene A as a promising insecticidal compound in a microbial metabolite screening. J. Antibiot. (Tokyo) 70(3), 272-276 (2017).

ABT-046 is an orally active, selective, and highly efficient Diacylglycerol Acyltransferase 1 (DGAT-1) inhibitor that can be used in metabolic disease research.

ALN29882 is a glycerolipid, that is located at the plasma membrane. It is made up of two fatty acid chains that are covalently attached to a single glycerol molecule with the help of an ester linkage. 18:1 DG has been used as a diacyl-glycerol source in diacylglycerol O-acyltransferase 1 (DGAT1) assay. It has also been used as substrate to assess compounds as potential inhibitors of DGAT-1 in DGAT-1 enzyme assay. It is suitable to use in lipid-protein overlay screen assay with the recombinant protein His-AtROP6.

DGAT1-IN-3 is a selective, potent, orally active DGAT-1 inhibitor that inhibits human DGAT-1 (IC50: 38 nM) and rat DGAT-1 (IC50: 120 nM).DGAT1-IN-3 can be used in studies of obesity, dyslipidemia and metabolic syndrome.