504924 | Indomethacin, 2ʹ-Trifluoromethyl - Calbiochem

504924
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₉H₁₃ClF₃NO₄

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.04924.0001
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          Glass bottle 10 mg
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          Description
          OverviewA 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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Blobaum, A.L., et al. 2013. ACS Med. Chem. Lett. 4, 486.
          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.

          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 +2°C to +8°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 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesBlobaum, A.L., et al. 2013. ACS Med. Chem. Lett. 4, 486.