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PF-06424439

  Cat. No.:  DC34453   Featured
Chemical Structure
1469284-78-3
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More than 5000 active chemicals with high quality for research!
Field of application
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 μM) against human MGAT2 or MGAT3, DGAT1, or mouse MGAT1, indicating a high selectivity (>2000-fold) against these enzymes.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1469284-78-3
Chemical Name: (R)-(1-(2-(1-(4-Chloro-1H-pyrazol-1-yl)cyclopropyl)-3H-imidazo[4,5-b]pyridin-5-yl)piperidin-3-yl)(pyrrolidin-1-yl)methanone
Synonyms: (R)-(1-(2-(1-(4-chloro-1H-pyrazol-1-yl)cyclopropyl)-3H-imidazo[4,5-b]pyridin-5-yl)piperidin-3-yl)(pyrrolidin-1-yl)methanone;BDBM215552;US9296745, 109-A;US9296745, 109-B;US9296745, 190;[(3R)-1-[2-[1-(4-chloropyrazol-1-yl)cyclopropyl]-1H-imidazo[4,5-b]pyridin-5-yl]piperidin-3-yl]-pyrrolidin-1-ylmethanone
SMILES: 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]
Formula: C22H26ClN7O
M.Wt: 439.9411
Purity: >98%
Sotrage: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
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].
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.
References: [1]. Futatsugi K, et al. Discovery and Optimization of Imidazopyridine-Based Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2). J Med Chem. 2015 Sep 24;58(18):7173-85. [2]. Pabst B, et al. Mechanistic Characterization of Long Residence Time Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2). Biochemistry. 2018 Dec 26;57(51):6997-7010.
MSDS
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COA
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