PF-06427878

PF-06427878 is an orally active, selective liver-targeted diacylglycerol acyltransferase 2 (DGAT2) inhibitor with IC50s of 99 nM and 202 nM for human and rat DGAT2, respectively. PF-06427878 shows greater than 470-fold selectivity for DGAT2 over DGAT1, MGAT1, MGAT2 and MGAT3. PF-06427878 can improve liver steatosis and function. PF-06427878 can be used for the study of nonalcoholic fatty liver diseases[1][2].

Product Specifications

CAS Number

[1809064-23-0]

UNSPSC

12352005

Target

Acyltransferase

Related Pathways

Metabolic Enzyme/Protease

Field of Research

Metabolic Disease; Inflammation/Immunology

Smiles

O=C(O)C1=CC=CC(CNC(C2=CN=C(N3C[C@H](OC4=CC=CC=C4OCC)CCC3)N=C2)=O)=C1

Molecular Formula

C26H28N4O5

Molecular Weight

476.52

References & Citations

[1]Sharma R, et al. Mitigating a Bioactivation Liability with an Azetidine-Based Inhibitor of Diacylglycerol Acyltransferase 2 (DGAT2) En Route to the Discovery of the Clinical Candidate Ervogastat. Chem Res Toxicol. 2023 Jun 19;36 (6) :934-946. |[2]Amin NB, et al. Targeting diacylglycerol acyltransferase 2 for the treatment of nonalcoholic steatohepatitis. Sci Transl Med. 2019 Nov 27;11 (520) :eaav9701.