PF-07247685

• Description:

  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].

• UNSPSC:

  12352005

• Target:

  Endogenous Metabolite

• Type:

  Reference compound

• Related Pathways:

  Metabolic Enzyme/Protease

• Applications:

  Neuroscience-Neuromodulation

• Field of Research:

  Cardiovascular Disease

• Assay Protocol:

  https://www.medchemexpress.com/pf-07247685.html

• Purity:

  98.66

• Solubility:

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

• Smiles:

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

• Molecular Formula:

  C21H20N2O3S

• Molecular Weight:

  380.46

• References & Citations:

  [1]Roth Flach RJ, et al. Small molecule branched-chain ketoacid dehydrogenase kinase (BDK) inhibitors with opposing effects on BDK protein levels. Nat Commun. 2023 Aug 9;14 (1) :4812.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported