PF-06471553

PF-06471553 is a potent, selective and orally available monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC50 of 92 nM.

Signaling Pathways >> Metabolic Enzyme/Protease >> Acyltransferase

Research Areas >> Metabolic Disease

IC50: 92 nM (MGAT3)[1]

PF-06471553 (6f) is a potent and selective monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC50 of 92 nM, and shows >160 fold in vitro selectivity for MGAT3 over DGAT1 (IC50, >50 μM), DGAT2 (IC50, >100 μM), MGAT1 (IC50, 14.9 μM), and MGAT2 (IC50, 19.8 μM). PF-06471553 exhibits inhibitory activity against MGAT3 in HEK-293 cells with an IC50 of 205 nM (pIC50, 6.69)[1].

PF-06471553 (200 mg/kg, p.o.) in addition with (DGAT1 and DGAT2) inhibitors shows additional inhibition of glycerol-d5 incorporated triolein in hMGAT3 mice, and with no effect on WT mice[1].

[1]. Huard K, et al. Discovery of Selective Small Molecule Inhibitors of Monoacylglycerol Acyltransferase 3. J Med Chem. 2015 Sep 24;58(18):7164-72.

Avasimibe | LCQ-908 | DGAT-3 | A922500 | Xanthohumol | PF-04620110 | AZD7687 | MGAT2-IN-1 | DGAT-1 inhibitor 2 | DGAT1-IN-1 | K-604 dihydrochloride | YM17E | ABT-046 | RP 70676 | Furan-2-carboxylic acid