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

533436
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Overview

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Key Spec Table

Empirical FormulaCAS #
C₂₁H₂₇N₅O₅S 496791-37-8

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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
      Quality LevelMQ100
      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 MSDS

      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.