1469284-79-4

PF-06424439 is an orally bioavailable inhibitor of diacylglycerol acyltransferase 2 (DGAT-2; IC₅₀ = 14 nM). It is selective for DGAT-2 over the related acyltransferases DGAT-1, MGAT-2, and MGAT-3 (IC₅₀s = >50 μM). PF-06424439 (0.1-10 mg/kg) reduces plasma triglyceride levels in sucrose-fed rats in a dose-dependent manner. It also reduces plasma levels of cholesterol and triglycerides as well as hepatic triglycerides in LDL receptor knockout mice fed a high-fat, high-cholesterol diet when administered at a dose of 60 mg/kg per day.

PF-06424439 has been used as a diacylglycerol acyltransferase 2 (DGAT2)?inhibitor:

• to study its effects on cell mortality and lipid synthesis in epithelial colon cells and colorectal cancer stem cells
• to study its effects on HeLa cells
• to study its inhibitory effects on neutral lipid synthesis in HT-1080 cells

PF-06424439 is a potent and selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2).

Store at -20°C

[1] KENTARO FUTATSUGI*. Discovery and Optimization of Imidazopyridine-Based Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2)[J]. Journal of Medicinal Chemistry, 2015, 58 18: 7173-7185. DOI: 10.1021/acs.jmedchem.5b01006
[2] A. NIKOLAI VON KRUSENSTIERN. Identification of essential sites of lipid peroxidation in ferroptosis[J]. Nature chemical biology, 2023, 19 6: 719-730. DOI: 10.1038/s41589-022-01249-3