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ProductsBack/AZD 7545 [252017-04-2]
Chemical Structure
Chemical Structure
Chemical Structure

AZD 7545 [252017-04-2]

Research Use Only
AG-CR1-3692
AdipoGen Life Sciences
CAS Number252017-04-2
DownloadMSDS
Product group Chemicals
Estimated Purity>98%
Molecular Weight478.9
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Overview

  • Supplier
    AdipoGen Life Sciences
  • Product Name
    AZD 7545 [252017-04-2]
  • Delivery Days Customer
    10
  • CAS Number
    252017-04-2
  • Certification
    Research Use Only
  • Estimated Purity
    >98%
  • Molecular Formula
    C19H18ClF3N2O5S
  • Molecular Weight
    478.9
  • Scientific Description
    Chemical. CAS: 252017-04-2. Formula: C19H18ClF3N2O5S. MW: 478.9. . Potent and selective pyruvate dehydrogenase kinase 2 (PDK2) inhibitor (IC50=6.4nM), consequently increasing pyruvate dehydrogenase (PDH) activity. Less potent inhibitor towards PDK1 and PDK3 (IC50=87 and 600nM, respectively). Inhibitor of glycolysis. Antiobesity and antidiabetic agent. Improves blood glucose control in obese (fa/fa) Zucker rats. Useful agent for immunometabolism research. To maintain a continuous and steady supply of ATP during the feed-fast cycle, cells must select fatty acid or glucose for fuel. This process is largely controlled by the pyruvate dehydrogenase complex (PDC), which regulates the entry of glycolytic products into the tricarboxylic acid cycle by catalyzing the oxidative decarboxylation of pyruvate to acetyl-coenzyme A (CoA) in the mitochondria of mammalian cells. PDKs and pyruvate dehydrogenase phosphatases (PDPs) are key regulators of PDC activity, and they act in a phosphorylation-dephosphorylation manner. - Potent and selective pyruvate dehydrogenase kinase 2 (PDK2) inhibitor (IC50=6.4nM), consequently increasing pyruvate dehydrogenase (PDH) activity. Less potent inhibitor towards PDK1 and PDK3 (IC50=87 and 600nM, respectively). Inhibitor of glycolysis. Antiobesity and antidiabetic agent. Improves blood glucose control in obese (fa/fa) Zucker rats. Useful agent for immunometabolism research. To maintain a continuous and steady supply of ATP during the feed-fast cycle, cells must select fatty acid or glucose for fuel. This process is largely controlled by the pyruvate dehydrogenase complex (PDC), which regulates the entry of glycolytic products into the tricarboxylic acid cycle by catalyzing the oxidative decarboxylation of pyruvate to acetyl-coenzyme A (CoA) in the mitochondria of mammalian cells. PDKs and pyruvate dehydrogenase phosphatases (PDPs) are key regulators of PDC activity, and they act in a phosphorylation-dephosphorylation manner.
  • SMILES
    O=C(N(C)C)C1=CC=C(S(C2=CC(Cl)=C(NC([C@](O)(C)C(F)(F)F)=O)C=C2)(=O)=O)C=C1
  • Storage Instruction
    -20°C,2°C to 8°C
  • UNSPSC
    12352200

References

  • AZD7545, a novel inhibitor of pyruvate dehydrogenase kinase 2 (PDHK2), activates pyruvate dehydrogenase in vivo and improves blood glucose control in obese (fa/fa) Zucker rats: R.M. Mayers, et al.; Biochem. Soc. Trans. 31, 1165 (2003)
  • AZD7545 is a selective inhibitor of pyruvate dehydrogenase kinase 2: J.A. Morrell, et al.; Biochem. Soc. Trans. 31, 1168 (2003)
  • Recognition of the inner lipoyl-bearing domain of dihydrolipoyl transacetylase and of the blood glucose-lowering compound AZD7545 by pyruvate dehydrogenase kinase 2: A. Tuganova, et al.; Biochem. 46, 8592 (2007)
  • Distinct Structural Mechanisms for Inhibition of Pyruvate Dehydrogenase Kinase Isoforms by AZD7545, Dichloroacetate, and Radicicol: M. Kato, et al.; Cell Structure 15, 992 (2007)
  • Dichloroacetate induces regulatory T-cell differentiation and suppresses Th17-cell differentiation by pyruvate dehydrogenase kinase-independent mechanism: N. Makita, et al.; J. Pharm. Pharmacol. 69, 43 (2017)