Name | PF-06424439 methanesulfonate |
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. |
Animal Research | 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]. |
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]. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 249 mg/mL (464.50 mM), Sonication is recommended. H2O : 99 mg/mL (184.68 mM)
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Keywords | acyl-CoA:cholesterol acyltransferase | Inhibitor | Acyltransferase | mono- acylglycerol acyltransferase | PF-06424439 | PF 06424439 methanesulfonate | inhibit | Diacylglycerol acyltransferase | PF06424439 | Diglyceride acyltransferase | PF06424439 methanesulfonate | PF 06424439 | PF-06424439 methanesulfonate |
Inhibitors Related | Serotonin hydrochloride | Risedronate Sodium | Cyclandelate | Risedronic Acid | YM17E | 3-Methoxybenzamide | Entacapone | 2-Furoic acid | OU749 | Ibandronate sodium | Alendronate sodium hydrate | Flopropione |
Related Compound Libraries | Bioactive Compound Library | Anti-Obesity Compound Library | Inhibitor Library | NO PAINS Compound Library | Lipid Metabolism Compound Library | Metabolism Compound Library | Orally Active Compound Library | Bioactive Compounds Library Max |