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539111 PAR-2 Agonist III

The PAR-2 Agonist III, also referenced under CAS 916170-19-9, controls the biological activity of PAR-2. This small molecule/inhibitor is primarily used for Activators/Inducers applications.

PAR-2 Agonist III : FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: (E)-N-((1-(3-Bromophenyl)-ethylidene-hydrazinocarbonyl)-(4-oxo-3,4-dihydro-phthalazin-1-yl)-methyl)-benzamide, AC-55541

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      Aperçu

      Replacement Information

      Tableau de caractéristiques principal

      CAS #Empirical Formula
      916170-19-9C₂₅H₂₀BrN₅O₃
      Description
      Overview

      This product has been discontinued.





      A cell-permeable, nonpeptidic phthalazinyl-hydrazide compound that induces cellular proliferation, PI hydrolysis, and Ca2+ mobilization (pEC50 = 6.7, 5.9, 6.6, in PAR-2-expressing NIH3T3, HEK 293T, and KNRK cultures, respectively) in a PAR-2-, but not PAR-1/3/4-, dependent manner, while exhibiting no significant affinity toward a panel of over 30 other receptors and channels implicated in nociception and inflammation. Shown to effectively elicit edema (by ~18%, 4 h after a direct injection dose of 30 ng/paw) and increased thermal hyperalgesia (by ~24% and ~85% drop in response time, respectively, 2 h after a direct injection dose of 30 ng/paw or an i.p. dose of 10 mg/kg) in rat models of acute inflammation and nociception in vivo. AC-55541 is metabolically stable (6 and 19 µl/min/mg, respectively, in human and rat liver microsome preparations) and pharmacokinetic studies reveal a peak plasma concentration of 1035 ng/ml at 50 min after an i.p. dose of 10 mg/kg and an elimination half-life of 6.1 h in rats in vivo.
      Catalogue Number539111
      Brand Family Calbiochem®
      Synonyms(E)-N-((1-(3-Bromophenyl)-ethylidene-hydrazinocarbonyl)-(4-oxo-3,4-dihydro-phthalazin-1-yl)-methyl)-benzamide, AC-55541
      References
      ReferencesGardell, L.R., et al. 2008. J. Pharmacol. Exp. Ther. 327, 799.
      Seitzberg, J.G., et al. 2008. J. Med. Chem. 51, 5490.
      Product Information
      CAS number916170-19-9
      FormWhite solid
      Hill FormulaC₂₅H₂₀BrN₅O₃
      Chemical formulaC₂₅H₂₀BrN₅O₃
      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
      S PhraseS: 22-24/25-36/37/39

      Do not breathe dust.
      Avoid contact with skin and eyes.
      Wear suitable protective clothing, gloves and eye/face protection.
      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 3 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
      539111 0

      Documentation

      PAR-2 Agonist III Certificats d'analyse

      TitreNuméro de lot
      539111

      Références bibliographiques

      Aperçu de la référence bibliographique
      Gardell, L.R., et al. 2008. J. Pharmacol. Exp. Ther. 327, 799.
      Seitzberg, J.G., et al. 2008. J. Med. Chem. 51, 5490.
      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.

      Revision19-July-2010 RFH
      Synonyms(E)-N-((1-(3-Bromophenyl)-ethylidene-hydrazinocarbonyl)-(4-oxo-3,4-dihydro-phthalazin-1-yl)-methyl)-benzamide, AC-55541
      DescriptionA cell-permeable, nonpeptidic phthalazinyl-hydrazide compound that induces cellular proliferation, PI hydrolysis, and Ca2+ mobilization (pEC50 = 6.7, 5.9, 6.6, in PAR-2-expressing NIH3T3, HEK 293T, and KNRK cultures, respectively) in a PAR-2-, but not PAR-1/3/4-, dependent manner, while exhibiting no significant affinity toward a panel of over 30 other receptors and channels implicated in nociception and inflammation. Shown to effectively elicit edema (by ~18%, 4 h after a direct injection dose of 30 ng/paw) and increased thermal hyperalgesia (by ~24% and ~85% drop in response time, respectively, 2 h after a direct injection dose of 30 ng/paw or an i.p. dose of 10 mg/kg) in rat models of acute inflammation and nociception in vivo. AC-55541 is metabolically stable (6 and 19 µl/min/mg, respectively, in human and rat liver microsome preparations) and pharmacokinetic studies reveal a peak plasma concentration of 1035 ng/ml at 50 min after an i.p. dose of 10 mg/kg and an elimination half-life of 6.1 h in rats in vivo.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number916170-19-9
      Chemical formulaC₂₅H₂₀BrN₅O₃
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (100 mg/ml). Sonication is required for complete solublization.
      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 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesGardell, L.R., et al. 2008. J. Pharmacol. Exp. Ther. 327, 799.
      Seitzberg, J.G., et al. 2008. J. Med. Chem. 51, 5490.