613810 TNAP Inhibitor - CAS 496014-13-2 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical FormulaCAS #
C₁₇H₁₆N₂O₄S 496014-13-2

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613810-10MG
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      10 mg
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      Description
      OverviewA cell-permeable quinolinyl-benzenesulfonamide compound that acts as a potent reversible inhibitor against tissue-nonspecific (TN) alkaline phosphatase (AP) activity (IC50 = 190 nM) with CYP2C19 being the only other known target, while exhibiting little or no inhibitory activity in over 250 assays involving other enzymes, including, but not limited to, placental and intestinal APs (IC50 > 100 µM), PHOSPHO1 phosphatase, and NPP1 phosphodiesterase. Kinetic studies indicate that the inhibition is uncompetitive with respect to the phosphate donor substrate and noncompetitive with respect to the acceptor substrate, indicating an allosteric inhibition mechanism. Subcutaneous dosing in rats in vivo is reported to result in plasma inhibitor concentrations in the therapeutic range (Cmax = 1.5 µg/ml 1 hr after 4.13 mg/kg by s.c.).
      Catalogue Number613810
      Brand Family Calbiochem®
      Synonyms2,5-Dimethoxy-N-(quinolin-3-yl)benzenesulfonamide, Tissue-Nonspecific Alkaline Phosphatase Inhibitor, MLS-0038949
      References
      ReferencesDahl, R., et al. 2009. J. Med. Chem. 52, 6919.
      Product Information
      CAS number496014-13-2
      FormWhite solid
      Hill FormulaC₁₇H₁₆N₂O₄S
      Chemical formulaC₁₇H₁₆N₂O₄S
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥95% by HPLC
      Physicochemical Information
      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 store at (4°C). Stock solutions are stable for up to 6 months at 4°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      TNAP Inhibitor - CAS 496014-13-2 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      TNAP Inhibitor - CAS 496014-13-2 - Calbiochem Certificates of Analysis

      TitleLot Number
      613810

      References

      Reference overview
      Dahl, R., et al. 2009. J. Med. Chem. 52, 6919.
      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.

      Revision19-April-2011 RFH
      Synonyms2,5-Dimethoxy-N-(quinolin-3-yl)benzenesulfonamide, Tissue-Nonspecific Alkaline Phosphatase Inhibitor, MLS-0038949
      DescriptionA cell-permeable quinolinyl-benzenesulfonamide compound that acts as a potent reversible inhibitor against tissue-nonspecific (TN) alkaline phosphatase (AP) activity (IC50 = 190 nM) with CYP2C19 being the only other known target, while exhibiting little or no inhibitory activity in over 250 assays involving other enzymes, including, but not limited to, placental and intestinal APs (IC50 >100 µM), PHOSPHO1 phosphatase, and NPP1 phosphodiesterase. Kinetic studies indicate that the inhibition is uncompetitive with respect to the phosphate donor substrate and noncompetitive with respect to the acceptor substrate, indicating an allosteric inhibition mechanism. Subcutaneous dosing in rats in vivo is reported to result in plasma inhibitor concentrations in the therapeutic range (Cmax = 1.5 µg/ml 1 hr after 4.13 mg/kg by s.c.).
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number496014-13-2
      Chemical formulaC₁₇H₁₆N₂O₄S
      Structure formulaStructure formula
      Purity≥95% 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 store at (4°C). Stock solutions are stable for up to 6 months at 4°C.
      Toxicity Standard Handling
      ReferencesDahl, R., et al. 2009. J. Med. Chem. 52, 6919.