PF-07238025

PF-07238025 is a BCKDC kinase (BDK) inhibitor (EC50=19 nM) . PF-07238025 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07238025 improved cardiometabolic endpoints and improves glucose tolerance in mice[1].

C19H18N2O3S

354.42

CC(C)COC(N=C1)=CC=C1C2=NC(C3=CC=CC=C3C(O)=O)=CS2

Endogenous Metabolite

99.46

DMSO : 100 mg/mL (ultrasonic)

-20°C, 3 years; 4°C, 2 years (Powder)

Room Temperature