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.

Product information

CAS Number: 1469284-78-3

Molecular Weight: 439.94

Formula: C22H26ClN7O

Chemical Name: (3R)-1-{2-[1-(4-chloro-1H-pyrazol-1-yl)cyclopropyl]-1H-imidazo[4, 5-b]pyridin-5-yl}-3-(pyrrolidine-1-carbonyl)piperidine

Smiles: O=C([C@H]1CN(CCC1)C1=CC=C2NC(=NC2=N1)C1(CC1)N1C=C(Cl)C=N1)N1CCCC1

InChiKey: PZHNKPBYOPQTRG-OAHLLOKOSA-N

InChi: InChI=1S/C22H26ClN7O/c23-16-12-24-30(14-16)22(7-8-22)21-25-17-5-6-18(26-19(17)27-21)29-11-3-4-15(13-29)20(31)28-9-1-2-10-28/h5-6,12,14-15H,1-4,7-11,13H2,(H,25,26,27)/t15-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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-/-). 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.

Products are for research use only. Not for human use.