| Description | PF-06424439 methanesulfonate, an orally administered, potent, and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM, demonstrates slow reversibility and time-dependent inhibition. It operates in a noncompetitive manner relative to the acyl-CoA substrate, marking its efficacy in targeting DGAT2. |
| In vivo | PF-06424439 methanesulfonate shows moderate clearance in rats following intravenous administration and moderate steady-state volume of distribution (Vdss) results in a short half-life[1]. |
| Animal experiments | PF-06424439 methanesulfonate (i.v.; 1 mg/kg) shows moderate clearance in rats following intravenous administration and moderate steady-state volume of distribution (Vdss) results in a short half-life[1].PF-06424439 methanesulfonate (p.o.; 60 mg/kg/day; for 3 days) reduces plasma TG and cholesterol levels and decreases nonsignificant in circulating lipids in mice (Ldlr-/-)[1]. |
| Target activity | DGAT-2:14 nM |
| molecular weight | 536.05 |
| Molecular formula | C23H30ClN7O4S |
| CAS | 1469284-79-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 249 mg/mL (464.50 mM), Sonication is recommended. H2O: 99 mg/mL (184.68 mM) |
| References | 1. Futatsugi K, et al. Discovery and Optimization of Imidazopyridine-Based Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2). J Med Chem. 2015 Sep 24;58(18):7173-85. 2. Pabst B, et al. Mechanistic Characterization of Long Residence Time Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2). Biochemistry. 2018 Dec 26;57(51):6997-7010. |
PF-06424439 methanesulfonate
CAS No.: 1469284-79-4
PF-06424439 methanesulfonate, an orally administered, potent, and selective imidazopyridine diacylglycerol acyltransfera
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