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

Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
496791-37-8C₂₁H₂₇N₅O₅S

Products

Catalog NumberPackaging Qty/Pack
5.33436.0001 Glass bottle 5 mg
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
FormWhite to brown 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
Global Trade Item Number
Catalog Number GTIN
5.33436.0001 04055977286922

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.

Revision30-November-2020 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.
FormWhite to brown solid
Intert gas (Yes/No) Packaged under inert gas
CAS number496791-37-8
Chemical formulaC₂₁H₂₇N₅O₅S
Purity≥95% by HPLC
SolubilityDMSO (100 mM)
Storage Protect from light
-20°C
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.