DGAT-1 inhibitor,potent and selective
CAS：1109276-89-2
分子式：C21H24N4O4
分子量：396.44
纯度：98%
存储：Store at -20°C

Background:

PF-04620110 is a potent, selective and orally-bioavailable inhibitor of diacylglycerol acyltransferase 1 (DGAT-1), an enzyme catalyzing the final committed step in the biosynthesis of triglycerides, that inhibits DGAT-1 with values of 50% inhibition concentration IC₅₀of 19 nM and 8 nM in human and HT-29 cells respectively. PF-04620110 displays a highly selective, more than 100 fold, inhibition against DGAT-1 rather than a range of lipid processing enzymes, including human DGAT-2, human acyl-CoA:cholesterol acyltransferase 1, human acyl-CoA:wax alcohol acyltransferase 1, human acyl-CoA:wax alcohol acyltransferase 2, human acyl-CoA:monacylglycerol acyltransferase 2, human acyl-CoA:monacylglycerol acyltransferase 3 and mouse MGAT 1.

Reference

Lee KR, Choi SH, Song JS, Seo H, Chae YJ, Cho HE, Ahn JH, Ahn SH, Bae MA. Determination of PF-04620110, a novel inhibitor of diacylglycerol acyltransferase-1, in rat plasma using liquid chromatography-tandem mass spectrometry and its application in pharmacokinetic studies. Biomed Chromatogr. 2013; 27(7):846-852.

Robert L. Dow *, Jian-Cheng Li , Michael P. Pence , E. Michael Gibbs , Jennifer L. LaPerle , John Litchfield , David W. Piotrowski , Michael J. Munchhof , Tara B. Manion , William J. Zavadoski , Gregory S. Walker , R. Kirk McPherson , Susan Tapley , Eliot Sugarman , Angel Guzman-Perez , and Paul DaSilva-Jardine Discovery of PF-04620110, a Potent, Selective, and Orally Bioavailable Inhibitor of DGAT-1. ACS Med. Chem. Lett., 2011, 2 (5), pp 407–412