533639 Pyruvate Dehydrogenase Kinase Inhibitor, AZD7545 - CAS 252017-04-2 - Calbiochem

533639
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Overview

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Key Specifications Table

Empirical FormulaCAS #
C₂₉H₂₈ClN₇OS 252017-04-2

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      Description
      OverviewA cell-permeable, bioavailable trifluomethylpropanamide compound that acts as a potent, selective, reversible, non-ATP-competitive inhibitor of pyruvate dehydrogenase kinases (IC50 = 36.8 & 6.4 nM for PDhK1 & PDhK2, respectively). Inhibits PDhK3 at much higher concentrations (IC50 = 600 nM) and robustly stimulates PDhK4 activity (> 10 nM). Also shown to increase pyruvate dehydrogenase (PDh) activity in liver and muscle, and potentiates pyruvate oxidation (EC50 = 105 nM in rat hepatocytes). Occupies lipoyl domain-binding site of PDhK2 (Kd = 19.2 nM) and disrupts the association of PDhK2 and inner lipoyl-bearing domain 2 of dihydrolipoyl acetyltransferase. Improves 24-h glucose profile and eliminates postparandial elevation in blood glucose in Zucker (fa/Fa) rats (10 mg/kg, b.i.d, p.o.,7 days).

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number533639
      Brand Family Calbiochem®
      SynonymsPDK Inhibitor, (R)-4-(3-Chloro-4-(3,3,3-trifluoro-2-hydroxy-2-methylpropanamido)phenylsulfonyl)-N,N-dimethylbenzamide, PDh Kinase Inhibitor, PDhK Inhibitor
      References
      ReferencesLi, J., et al. 2009. J. Biol. Chem. 284, 34458.
      Tuganova, A., et al. 2007. Biochemistry 46, 8592.
      Morrell, J.A., et al. 2003. Biochem. Soc. Trans. 31, 1168.
      Mayers, R.M., et al. 2003. Biochem. Soc. Trans. 31, 1165.
      Product Information
      CAS number252017-04-2
      FormWhite solid
      Hill FormulaC₂₉H₂₈ClN₇OS
      Chemical formulaC₂₉H₂₈ClN₇OS
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary Targetpyruvate dehydrogenase kinases
      Primary Target IC<sub>50</sub>36.8 & 6.4 nM for PDhK1 & PDhK2, respectively
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Pyruvate Dehydrogenase Kinase Inhibitor, AZD7545 - CAS 252017-04-2 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Li, J., et al. 2009. J. Biol. Chem. 284, 34458.
      Tuganova, A., et al. 2007. Biochemistry 46, 8592.
      Morrell, J.A., et al. 2003. Biochem. Soc. Trans. 31, 1168.
      Mayers, R.M., et al. 2003. Biochem. Soc. Trans. 31, 1165.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision20-November-2015 JSW
      SynonymsPDK Inhibitor, (R)-4-(3-Chloro-4-(3,3,3-trifluoro-2-hydroxy-2-methylpropanamido)phenylsulfonyl)-N,N-dimethylbenzamide, PDh Kinase Inhibitor, PDhK Inhibitor
      DescriptionA cell-permeable, bioavailable trifluomethylpropanamide compound that acts as a potent, selective, reversible, non-ATP-competitive inhibitor of pyruvate dehydrogenase kinases (IC50 = 36.8 & 6.4 nM for PDhK1 & PDhK2, respectively). Inhibits PDhK3 at much higher concentrations (IC50 = 600 nM) and robustly stimulates PDhK4 activity (> 10 nM). Also shown to increase pyruvate dehydrogenase (PDh) activity in liver and muscle, and potentiates pyruvate oxidation (EC50 = 105 nM in rat hepatocytes). Occupies lipoyl domain-binding site of PDhK2 (Kd = 19.2 nM) and disrupts the association of PDhK2 and inner lipoyl-bearing domain 2 of dihydrolipoyl acetyltransferase. Improves 24-h glucose profile and eliminates postparandial elevation in blood glucose in Zucker (fa/Fa) rats (10 mg/kg, b.i.d, p.o.,7 days).
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number252017-04-2
      Chemical formulaC₂₉H₂₈ClN₇OS
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesLi, J., et al. 2009. J. Biol. Chem. 284, 34458.
      Tuganova, A., et al. 2007. Biochemistry 46, 8592.
      Morrell, J.A., et al. 2003. Biochem. Soc. Trans. 31, 1168.
      Mayers, R.M., et al. 2003. Biochem. Soc. Trans. 31, 1165.