PF-07247685

PF-07247685 is a BCKDC kinase (BDK) inhibitor (EC50=2.2 nM) . PF-07247685 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-07247685 improved cardiometabolic endpoints and improves glucose tolerance in mice[1].

C21H20N2O3S

380.46

O=C(O)C1=CC=CC=C1C2=NC(C3=CC=C(OCC4(CC4)CC)N=C3)=CS2

Endogenous Metabolite

98.66

DMSO : 100 mg/mL (ultrasonic) |Ethanol : 100 mg/mL (ultrasonic)

-20°C, 3 years; 4°C, 2 years (Powder)

Room Temperature