PF-06424439 methanesulfonate

SKU: orb1309264

Description

PF-06424439 methanesulfonate is a potent and selective DGAT2 inhibitor with an IC50 of 14 nM. This orally available, noncompetitive, and slowly reversible inhibitor is used in research to investigate lipid metabolism in both in vitro and in vivo models, particularly for metabolic and liver disease studies.

Research Area

Metabolism Research

Key Properties

• CAS Number: 1469284-79-4
• MW: 536.05
• Purity: 99.77% (May vary between batches)
• Formula: C₂₃H₃₀ClN₇O₄S
• SMILES: CS(O)(=O)=O.Clc1cnn(c1)C1(CC1)c1nc2ccc(nc2[nH]1)N1CCC[C@H](C1)C(=O)N1CCCC1
• Target: Transferase|||Acyltransferase
• Solubility: H2O:99 mg/mL (184.68 mM);DMSO:262.5 mg/mL (489.69 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (9.33 mM)

Bioactivity

• Target 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.
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• 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.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-/-).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

mono- acylglycerol acyltransferase, Inhibitor, inhibit, Acyltransferase, acyl-CoA:cholesterol acyltransferase, DGAT2, Diacylglycerol acyltransferase, Diglyceride acyltransferase, PF 06424439, PF 06424439 methanesulfonate, PF06424439, PF-06424439, PF06424439 methanesulfonate, PF-06424439 methanesulfonate

Compound Identifiers

PubChem CID

89854212