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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $39 | In Stock | |
5 mg | $55 | In Stock | |
10 mg | $97 | In Stock | |
25 mg | $197 | In Stock | |
50 mg | $328 | In Stock | |
100 mg | $538 | In Stock | |
1 mL x 10 mM (in DMSO) | $66 | In Stock |
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. |
Targets&IC50 | DGAT-2:14 nM |
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 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]. |
Molecular Weight | 536.05 |
Formula | C23H30ClN7O4S |
Cas No. | 1469284-79-4 |
Smiles | CS(O)(=O)=O.Clc1cnn(c1)C1(CC1)c1nc2ccc(nc2[nH]1)N1CCC[C@H](C1)C(=O)N1CCCC1 |
Relative Density. | no data available |
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) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
H2O/DMSO
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