PF-07208254

Overview

PF-07208254 is a selective, orally active allosteric inhibitor of branched-chain ketoacid dehydrogenase kinase (BDK) (IC 50 =110 nM, K i =54 nM, K D =84 nM). PF-07208254 inhibits BDK-mediated BCKDH phosphorylation and enhances the catabolism of branched-chain amino acids (BCAAs) and branched-chain keto acids (BCKAs) by binding to the allosteric pocket of BDK, reducing BDK binding to BCKDH-E2 and promoting BDK degradation. PF-07208254 inhibits BDK activity in human skeletal muscle cells (IC 50 =540 nM) and has activity to improve cardiac function and metabolism. PF-07208254 can be used in the study of cardiometabolic diseases (e.g., heart failure, type 2 diabetes).

Application

Products | Products > Disease Areas > Blood or Cardio-cerebrovascular Disease | Products > Disease Areas > Metabolic or Endocrine Disease | Products > Signaling Pathways > Metabolic Enzyme/Protease | Products > Research Areas > Metabolic Disease | Products > Research Areas > Cardiovascular Disease | Products > Signaling Pathways > PDHK

Product Information

• Catalog No.: HY-156193
• CAS No.: 2573122-40-2
• Molecular Formula: C7H2ClFO2S2
• Molecular Weight: 236.67
• Purity: 98.46%
• Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
• Solubility: 2.5 mg/mL (10.56 mM); Clear solution; Need ultrasonic
• Availability: In-stock

Source

Original product source