1. Metabolic Enzyme/Protease
  2. Acyltransferase
  3. PF-06424439

PF-06424439 

Cat. No.: HY-108341
Handling Instructions

PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM. PF-06424439 is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate.

For research use only. We do not sell to patients.

PF-06424439 Chemical Structure

PF-06424439 Chemical Structure

CAS No. : 1469284-78-3

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Description

PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM[1]. PF-06424439 is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate[2].

IC50 & Target

IC50: 14 nM (DGAT2)[1]

In Vivo

PF-06424439 (p.o.; 60 mg/kg/day; for 3 days) reduces plasma triglyceride (TG) and cholesterol levels and decreases nonsignificant in circulating lipids in mice (Ldlr-/-)[1].
PF-06424439 (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].

Animal Model: Male low-density lipoprotein receptor (Ldlr) knockout mice (Ldlr-/-)[1]
Dosage: 60 mg/kg
Administration: P.o.; daily; for 3 days
Result: Reduced plasma TG and cholesterol levels and decreased nonsignificant in circulating lipids.
Animal Model: Male Wistar-Han rats[1]
Dosage: 1 mg/kg
Administration: I.v.
Result: Showed moderate clearance and a short half-life with t1/2=1.39 h.
Molecular Weight

439.94

Formula

C₂₂H₂₆ClN₇O

CAS No.

1469284-78-3

SMILES

O=C([[email protected]]1CN(C2=CC=C3C(NC(C4(N5N=CC(Cl)=C5)CC4)=N3)=N2)CCC1)N6CCCC6

Shipping

Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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PF-06424439
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HY-108341
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