PF-06471553 is a potent, selective and orally available monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC 50 of 92 nM.
In Vitro
PF-06471553 (6f) is a potent and selective monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC 50 of 92 nM, and shows >160 fold in vitro selectivity for MGAT3 over DGAT1 (IC 50 , >50 μM), DGAT2 (IC 50 , >100 μM), MGAT1 (IC 50 , 14.9 μM), and MGAT2 (IC 50 , 19.8 μM). PF-06471553 exhibits inhibitory activity against MGAT3 in HEK-293 cells with an IC 50 of 205 nM (pIC 50 , 6.69). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
