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PF-06424439 methanesulfonate

Catalog No. T12425 CAS 1469284-79-4

PF-06424439 methanesulfonate, an orally administered, potent, and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM, demonstrates slow reversibility and time-dependent inhibition. It operates in a noncompetitive manner relative to the acyl-CoA substrate, marking its efficacy in targeting DGAT2.

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PF-06424439 methanesulfonate Chemical Structure

PF-06424439 methanesulfonate, CAS 1469284-79-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 39.00
5 mg	In stock	$ 55.00
10 mg	In stock	$ 97.00
25 mg	In stock	$ 197.00
50 mg	In stock	$ 328.00
100 mg	In stock	$ 538.00
1 mL * 10 mM (in DMSO)	In stock	$ 66.00

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Purity: 99.79%

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Description	PF-06424439 methanesulfonate, an orally administered, potent, and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM, demonstrates slow reversibility and time-dependent inhibition. It operates in a noncompetitive manner relative to the acyl-CoA substrate, marking its efficacy in targeting DGAT2.
Targets&IC50	DGAT-2:14 nM
In vivo	PF-06424439 methanesulfonate shows moderate clearance in rats following intravenous administration and moderate steady-state volume of distribution (Vdss) results in a short half-life[1].
Animal Research	PF-06424439 methanesulfonate (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].PF-06424439 methanesulfonate (p.o.; 60 mg/kg/day; for 3 days) reduces plasma TG and cholesterol levels and decreases nonsignificant in circulating lipids in mice (Ldlr-/-)[1].

Molecular Weight	536.05
Formula	C23H30ClN7O4S
CAS No.	1469284-79-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 249 mg/mL (464.50 mM), Sonification is recommended.

H2O: 99 mg/mL (184.68 mM)

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Metabolism Compound Library Lipid Metabolism Compound Library Anti-Obesity Compound Library Bioactive Compound Library NO PAINS Compound Library Bioactive Compounds Library Max Orally Active Compound Library

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Keywords

PF-06424439 methanesulfonate 1469284-79-4 Metabolism Transferase Acyltransferase acyl-CoA:cholesterol acyltransferase Inhibitor mono- acylglycerol acyltransferase PF-06424439 PF 06424439 methanesulfonate inhibit Diacylglycerol acyltransferase PF06424439 Diglyceride acyltransferase PF06424439 methanesulfonate PF 06424439 inhibitor

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