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PF-06424439 methanesulfonate

Catalog No. T12425Cas No. 1469284-79-4

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.

PF-06424439 methanesulfonate

PF-06424439 methanesulfonate

Purity: 99.77%
Catalog No. T12425Cas No. 1469284-79-4
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 SizePriceAvailabilityQuantity
1 mg$39In Stock
5 mg$55In Stock
10 mg$97In Stock
25 mg$197In Stock
50 mg$328In Stock
100 mg$538In Stock
1 mL x 10 mM (in DMSO)$66In Stock
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Purity:99.77%
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Product Introduction

Bioactivity
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].
Chemical Properties
Molecular Weight536.05
FormulaC23H30ClN7O4S
Cas No.1469284-79-4
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM1.8655 mL9.3275 mL18.6550 mL93.2749 mL
5 mM0.3731 mL1.8655 mL3.7310 mL18.6550 mL
10 mM0.1865 mL0.9327 mL1.8655 mL9.3275 mL
20 mM0.0933 mL0.4664 mL0.9327 mL4.6637 mL
50 mM0.0373 mL0.1865 mL0.3731 mL1.8655 mL
100 mM0.0187 mL0.0933 mL0.1865 mL0.9327 mL

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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