533436 Monocarboxylate Transport Inhibitor, AR-C155858 - CAS 496791-37-8 - Calbiochem

533436
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₁H₂₇N₅O₅S 496791-37-8

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      5.33436.0001
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          Glass bottle 5 mg
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          Description
          OverviewA cell-permeable thieno[2,3-d]pyrimidinedione compound that acts as a highly potent inhibitor of monocarboxylate transporter 1 (MCT1; Ki = 2.3 nM for lactate uptake in rat erythrocytes). Also shown to inhibit MCT2 when associated with basigin (IC50 = 10 nM). Does not affect the activity of MCT4 even at higher concentration. Also shown to block MCT1 expressed in Xenopus oocytes Binds to MCT1 from the intracellular side involving transmembrane helices 7-10. Its inhibitory effect is significantly reduced with either F360Y or S364G mutations (~100 nM) and the inhibitory effect is lost with both sites are mutated (~5 µM). Displays high metabolic stability and low inhibition of CYP. Shown to block lactate transport and increase intracellular lactate levels in Raji Burkitt and MCF-7 cells and reduces their proliferation.

          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 Number533436
          Brand Family Calbiochem®
          Synonyms(S)-6-((3,5-dimethyl-1H-pyrazol-4-yl)methyl)-5-(4-hydroxyisoxazolidine-2-carbonyl)-1-isobutyl-3-methylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione , Monocarboxylate transporter 1 inhibitor, AR-C155858, SR13801
          References
          ReferencesNancolas, B., et al. 2015. Biochem. J. 467, 192.
          Ovens, M. J. et al. 2010. Biochem. J. 425, 523.
          Guile, S. D., et al. 2007. J. Med. Chem. 50, 254.
          Product Information
          CAS number496791-37-8
          FormBrown solid
          Hill FormulaC₂₁H₂₇N₅O₅S
          Chemical formulaC₂₁H₂₇N₅O₅S
          ReversibleY
          Applications
          Biological Information
          Primary TargetMCT1
          Primary Target K<sub>i</sub>1.2 nM
          Purity≥95% 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
          Toxicity Standard Handling
          Storage -20°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

          Monocarboxylate Transport Inhibitor, AR-C155858 - CAS 496791-37-8 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Nancolas, B., et al. 2015. Biochem. J. 467, 192.
          Ovens, M. J. et al. 2010. Biochem. J. 425, 523.
          Guile, S. D., et al. 2007. J. Med. Chem. 50, 254.
          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
          Synonyms(S)-6-((3,5-dimethyl-1H-pyrazol-4-yl)methyl)-5-(4-hydroxyisoxazolidine-2-carbonyl)-1-isobutyl-3-methylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione , Monocarboxylate transporter 1 inhibitor, AR-C155858, SR13801
          DescriptionA cell-permeable thieno[2,3-d]pyrimidinedione compound that acts as a highly potent inhibitor of monocarboxylate transporter 1 (MCT1; Ki = 2.3 nM for lactate uptake in rat erythrocytes). Also shown to inhibit MCT2 when associated with basigin (IC50 = 10 nM). Does not affect the activity of MCT4 even at higher concentration. Also shown to block MCT1 expressed in Xenopus oocytes Binds to MCT1 from the intracellular side involving transmembrane helices 7-10. Its inhibitory effect is significantly reduced with either F360Y or S364G mutations (~100 nM) and the inhibitory effect is lost with both sites are mutated (~5 µM). Displays high metabolic stability and low inhibition of CYP. Shown to block lactate transport and increase intracellular lactate levels in Raji Burkitt and MCF-7 cells and reduces their proliferation.
          FormBrown solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number496791-37-8
          Chemical formulaC₂₁H₂₇N₅O₅S
          Purity≥95% by HPLC
          SolubilityDMSO (50 mg/ml)
          Storage -20°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
          ReferencesNancolas, B., et al. 2015. Biochem. J. 467, 192.
          Ovens, M. J. et al. 2010. Biochem. J. 425, 523.
          Guile, S. D., et al. 2007. J. Med. Chem. 50, 254.