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

613810
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₇H₁₆N₂O₄S 496014-13-2

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      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
          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.