1808094-07-6

1808094-07-6 structure

Name: PF-06471553
Chemical Name: PF-06471553
CAS Number: 1808094-07-6
Molecular Formula: C₂₃H₂₅N₅O₄S
Molecular Weight: 467.54
Catalog: Signaling Pathways Metabolic Enzyme/Protease Acyltransferase
Create Date: 2018-09-05 23:52:32
Modify Date: 2024-01-03 13:15:20
PF-06471553 is a potent, selective and orally available monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC50 of 92 nM.

Name	PF-06471553

Description	PF-06471553 is a potent, selective and orally available monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC50 of 92 nM.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Acyltransferase Research Areas >> Metabolic Disease
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].
References	[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.