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

533639
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₉H₂₈ClN₇OS 252017-04-2

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      5.33639.0001
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          Glass bottle 5 mg
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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
          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.