PF-06424439

Biorbyt

PF-06424439 [1469284-78-3]

10

1469284-78-3

Research Use Only

C22H26CLN7O

439.9411

PF-06424439 is a potent and selective Diacylglycerol Acyltransferase 2 ( DGAT2) inhibitor with DGAT2 IC50 +/- SEM (nM) (human/rat/dog) 14 +/- 1/38 +/- 4/16 +/- 1. PF-06424439 demonstrated excellent ADMET properties and decreased circulating and hepatic lipids when orally administered to dyslipidemic rodent models. PF-06424439 inhibited DGAT2 of different species (human, rat, and dog) with similar potency. Among related acyltransferases, no significant inhibition was observed for PF-06424439 (up to 50 microM) against human MGAT2 or MGAT3, DGAT1, or mouse MGAT1, indicating a high selectivity (>2000-fold) against these enzymes.

ClC1C([H])=NN(C=1[H])C1(C2=NC3=C(C([H])=C([H])C(=N3)N3C([H])([H])C([H])([H])C([H])([H])[C@@]([H])(C(N4C([H])([H])C([H])([H])C([H])([H])C4([H])[H])=O)C3([H])[H])N2[H])C([H])([H])C1([H])[H]

12352200