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PF-06424439 (methanesulfonate)

PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM[1]. PF-06424439 methanesulfonate is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate[2].

Product Specifications

CAS Number

[1469284-79-4]

UNSPSC

12352005

Target

Acyltransferase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/pf-06424439-methanesulfonate.html

Purity

99.85

Solubility

DMSO : 250 mg/mL (ultrasonic) |H2O : 50 mg/mL (ultrasonic)

Smiles

O=C([C@H]1CN(C2=CC=C3C(NC(C4(N5N=CC(Cl)=C5)CC4)=N3)=N2)CCC1)N6CCCC6.CS(=O)(O)=O

Molecular Formula

C23H30ClN7O4S

Molecular Weight

536.05

References & Citations

[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.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Citation 01

Adv Sci (Weinh) . 2025 May 14:e2406150.|Anal Chem. 2025 Jul 22;97 (28) :15393-15401.|Biochim Biophys Acta Mol Cell Biol Lipids. 2025 Aug 22;1870 (8) :159683.|Int Immunopharmacol. 2024 Jun 24:138:112518.|J Biol Chem. 2024 Apr;300 (4) :107168.|J Dairy Sci. 2022 Apr;105 (4) :3588-3600.|J Dairy Sci. 2024 Jun 6:S0022-0302 (24) 00897-X.|J Virol. 2022 Jan 26;96 (2) :e0147321.|Mol Metab. 2024 Jun:84:101953.|bioRxiv. 2023 Jul 3.|bioRxiv. 2025 Jul 21.|bioRxiv. 2025 Mar 11:2025.02.18.638929.|Cell Death Dis. 2025 Oct 7;16 (1) :715.|Dev Comp Immunol. 2021 Nov:124:104197.|FASEB J. 2025 Nov 30;39 (22) :e71249.|Int J Biol Macromol. 2024 Dec;282 (Pt 5) :137235.|Nat Commun. 2024 Sep 27;15 (1) :8273.|Protein Cell. 2025 Nov 19:pwaf101.|Research Square Preprint. 2024 Feb 12.|Theranostics. 2024 Jun 1;14 (9) :3470-3485.

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