PF-04620110

PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.IC50 value: 19 nM [1]Target: DGAT1PF-04620110 and imipramine (internal standard) were separated using a Hypersil Gold C18 column, with a mixture of acetonitrile and 10 mm ammonium formate (90:10, v/v) as the mobile phase. The ion transitions monitored in positive-ion mode [M + H](+) of multiple-reaction monitoring were m/z 397.0 -260.2 for PF-04620110 and m/z 280.8 - 86.0 for imipramine. The detector response was specific and linear for PF-04620110 at concentrations within the range 0.05-50 μg/mL and the signal-to-noise ratios for the samples were ≥10 [2].

Signaling Pathways >> Metabolic Enzyme/Protease >> Acyltransferase

Research Areas >> Metabolic Disease

[1]. 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.

[2]. Lee KR, et al. 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 Jul;27(7):846-52

Avasimibe | LCQ-908 | DGAT-3 | A922500 | Xanthohumol | AZD7687 | MGAT2-IN-1 | DGAT-1 inhibitor 2 | DGAT1-IN-1 | K-604 dihydrochloride | PF-06471553 | YM17E | ABT-046 | RP 70676 | Furan-2-carboxylic acid