PF-06424439 (methanesulfonate)

• UNSPSC Description:

  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].

• Target Antigen:

  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 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.Int Immunopharmacol. 2024 Jun 24:138:112518.|J Biol Chem. 2024 Mar 13:107168.|J Dairy Sci. 2022 Feb 15;S0022-0302(22)00089-3.|J Dairy Sci. 2024 Jun 6:S0022-0302(24)00897-X.|J Virol. 2021 Nov 10;JVI0147321.|Mol Metab. 2024 May 4:101953.|bioRxiv. 2023 Jul 3.|Dev Comp Immunol. 2021 Jul 3;104197.|Int J Biol Macromol. 2024 Nov 3:137235.|Nat Commun. 2024 Sep 27;15(1):8273.|Research Square Preprint. 2024 Feb 12.|Theranostics. 2024 Jun 1;14(9):3470-3485.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

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

• Clinical Information:

  No Development Reported

• CAS Number:

  1469284-79-4