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].
Product Specifications
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
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Available Sizes
Frequently Asked Questions
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