tcsc0028403 PF-06471553

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

IC50 & Target: IC50: 92 nM (MGAT3)^[1]

In Vitro: 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].

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^[1].