PF-06424439

Product Name: PF-06424439
CAS No.: 1469284-78-3
Chemical Name: PF-06424439
Synonyms: Methanone, [(3R)-1-[2-[1-(4-chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinyl-;PF06424439,Diglyceride acyltransferase,mono- acylglycerol acyltransferase,Inhibitor,acyl-CoA:cholesterol acyltransferase,Diacylglycerol acyltransferase,PF 06424439,PF-06424439,Acyltransferase,inhibit
CBNumber: CB53355456
Molecular Formula: C22H26ClN7O
Formula Weight: 439.94
MOL File: 1469284-78-3.mol

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PF-06424439 Property

Boiling point:: 752.8±60.0 °C(Predicted)
Density: 1.57±0.1 g/cm3(Predicted)
solubility: DMSO:70.0(Max Conc. mg/mL);159.11(Max Conc. mM)
H2O:70.0(Max Conc. mg/mL);159.11(Max Conc. mM)
pka: 12.11±0.40(Predicted)

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Hazard and Precautionary Statements (GHS)

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PF-06424439 Chemical Properties,Usage,Production

Description

PF-06424439 is a potent and selective Diacylglycerol Acyltransferase 2 ( DGAT2) inhibitor with DGAT2 IC50 ± SEM (nM) (humarat/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.

in vitro

The effect of PF-06424439, a selective DGAT2 inhibitor, on MCF7 breast cancer cells exposed to X-rays was evaluated. The results demonstrated that 72 h of PF-06424439 treatment reduced LD (lipid droplets) content and inhibited cell migration, without affecting cell proliferation. Interestingly, PF-06424439 pre-treatment followed by radiation was able to enhance radiosensitivity of MCF7 cells. These findings suggest that PF-06424439 pre-treatment coupled to X-ray exposure might potentiate breast cancer cell radiosensitivity and potentially improve the radiotherapy effectiveness. _x000D_ _x000D_ Reference: Int J Mol Sci. 2021 Sep 18;22(18):10102. https://pubmed.ncbi.nlm.nih.gov/34576263/

in vivo

The effects of DGAT1 and DGAT2 inhibition, alone or in combination, on dietary TAG absorption and diarrhea in mice were investigated by using a selective DGAT1 inhibitor (PF-04620110) and DGAT2 inhibitor (PF-06424439). To further understand relationship between diarrhea and changes in DGAT activity, we examined dose‐dependent effects of DGAT inhibitors in mice. Simultaneous administration of a lower‐dose DGAT1 (0.03 mg/kg) inhibitor, which did not produce maximal effects on intestinal TAG secretion, and the DGAT2 inhibitors significantly decreased plasma radioactivity. These findings suggest that DGAT-mediated intestinal TAG synthesis is a vital step for maintaining intestinal barrier integrity under HFD (high-fat diet) feeding._x000D_ _x000D_ Reference: Physiol Rep. 2020 Aug;8(15):e14542. https://pubmed.ncbi.nlm.nih.gov/32786057/

target

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

PF-06424439 Preparation Products And Raw materials

Raw materials

Preparation Products

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PF-06424439 Suppliers

China 8 United States 3 Global 11

Jinan elephant international trading co., LTD

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Fan De(Beijing) Biotechnology Co., Ltd.

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TargetMol Chemicals Inc.

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DC Chemicals

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Nantong Hi-Future Biotechnology Co., Ltd

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TargetMol Chemicals Inc.

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Suzhou Zhixin Biotechnology Co., Ltd.

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Nanjing Shizhou Biology Technology Co.,Ltd

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Methanone, [(3R)-1-[2-[1-(4-chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinyl-

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

1469284-78-3