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504924 Indomethacin, 2ʹ-Trifluoromethyl - Calbiochem

504924
  
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      Aperçu

      Replacement Information

      Tableau de caractéristiques principal

      Empirical Formula
      C₁₉H₁₃ClF₃NO₄
      Description
      Overview

      This product has been discontinued.



      A cell-permeable, bioavailable 2′-trifluoromethyl analog of Indomethacin (Cat. No. 405268) that acts as a highly potent, time-dependent inhibitor of cyclooxygenase -2 (COX-2; IC50 = 267 and 388 nM for mouse and human COX-2, respectively) and its several mutant forms. Does not affect COX-1 activity even at high concentrations (IC50 >100 µM). Interacts with human COX-2 with much greater affinity than indomethacin (KI = 1.5 vs 13 µM) and blocks COX-2 dependent arachidonic acid oxygenation (IC50 = 150 nM in 1483 human head and neck squamous cell carcinoma cells). Further, minimizes swelling in carrageenan-induced rat paw edema model (EC50 = 1.7 mg/kg, p.o.) with no gastrointestinal bleeding at higher doses (10 mg/kg).

      Catalogue Number504924
      Brand Family Calbiochem®
      SynonymsIndomethacin, 2ʹ-Trifluoromethyl; Indomethacin, 2-CF₃, CF₃-Indomethacin; CF₃-INDO
      References
      ReferencesBlobaum, A.L., et al. 2013. ACS Med. Chem. Lett. 4, 486.
      Product Information
      FormWhite powder
      Hill FormulaC₁₉H₁₃ClF₃NO₄
      Chemical formulaC₁₉H₁₃ClF₃NO₄
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetCOX-2
      Primary Target IC<sub>50</sub>267 and 388 nM for mouse and human COX-2, respectively
      Purity≥98% 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 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 freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      504924 0

      Documentation

      Indomethacin, 2ʹ-Trifluoromethyl - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Blobaum, A.L., et al. 2013. ACS Med. Chem. Lett. 4, 486.
      Fiche technique

      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.

      Revision18-October-2013 JSW
      SynonymsIndomethacin, 2ʹ-Trifluoromethyl; Indomethacin, 2-CF₃, CF₃-Indomethacin; CF₃-INDO
      DescriptionA cell-permeable, bioavailable 2′-trifluoromethyl analog of Indomethacin (Cat. No. 405268) that acts as a highly potent, time-dependent inhibitor of cyclooxygenase -2 (COX-2; IC50 = 267 and 388 nM for mouse and human COX-2, respectively) and its several mutant forms. Does not affect COX-1 activity even at high concentrations (IC50 >100 µM). Interacts with human COX-2 with much greater affinity than indomethacin (KI = 1.5 vs 13 µM) and blocks COX-2 dependent arachidonic acid oxygenation (IC50 = 150 nM in 1483 human head and neck squamous cell carcinoma cells). Further, minimizes swelling in carrageenan-induced rat paw edema model (EC50 = 1.7 mg/kg, p.o.) with no gastrointestinal bleeding at higher doses (10 mg/kg).
      FormWhite powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₉H₁₃ClF₃NO₄
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesBlobaum, A.L., et al. 2013. ACS Med. Chem. Lett. 4, 486.