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236005 COX-1 Inhibitor, FR122047 - CAS 130717-51-0 - Calbiochem

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CAS #Empirical Formula
130717-51-0C₂₃H₂₅N₃O₃S • HCl

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236005-5MG
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      Description
      OverviewA cell-permeable trisubstituted thiazole compound that acts as a potent and selective inhibitor of COX-1 (IC50 = 28 nM and 65 µM for human recombinant COX-1 and COX-2, respectively). Displays ~2,300 fold greater selectivity towards inhibition of COX-1 over COX-2. Reported to be orally active and display analgesic, anti-platelet and anti-inflammatory properties.
      Catalogue Number236005
      Brand Family Calbiochem®
      SynonymsFR 122047, 1-[(4,5-Bis(4-methoxyphenyl-2-thiazoyl)carbonyl]-4-methylpiperazine, Hydrochloride, 4,5-Bis(4-methoxyphenyl-2-[(1-methylpiperazin-4-yl)carbonyl]thiazole, Hydrochloride
      References
      ReferencesOchi, T., and Goto, T. 2002. Br. J. Pharmacol. 135, 782.
      Ochi, T., et al. 2000. Eur. J. Pharmacol. 391, 49.
      Tanaka, A., et al. 1994. J. Med. Chem. 37, 1189.
      Dohi, M., et al. 1993. Eur. J. Pharmacol. 243, 179.
      Product Information
      CAS number130717-51-0
      ATP CompetitiveN
      FormPale yellow solid
      Hill FormulaC₂₃H₂₅N₃O₃S • HCl
      Chemical formulaC₂₃H₂₅N₃O₃S • HCl
      Hygroscopic Hygroscopic
      ReversibleN
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetCOX-1, COX-2
      Primary Target IC<sub>50</sub>28 nM and 65 µM for human recombinant COX-1 and COX-2
      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
      Hygroscopic Hygroscopic
      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
      236005-5MG 04055977217100

      Documentation

      COX-1 Inhibitor, FR122047 - CAS 130717-51-0 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      COX-1 Inhibitor, FR122047 - CAS 130717-51-0 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      236005

      Références bibliographiques

      Aperçu de la référence bibliographique
      Ochi, T., and Goto, T. 2002. Br. J. Pharmacol. 135, 782.
      Ochi, T., et al. 2000. Eur. J. Pharmacol. 391, 49.
      Tanaka, A., et al. 1994. J. Med. Chem. 37, 1189.
      Dohi, M., et al. 1993. Eur. J. Pharmacol. 243, 179.
      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.

      Revision12-June-2008 RFH
      SynonymsFR 122047, 1-[(4,5-Bis(4-methoxyphenyl-2-thiazoyl)carbonyl]-4-methylpiperazine, Hydrochloride, 4,5-Bis(4-methoxyphenyl-2-[(1-methylpiperazin-4-yl)carbonyl]thiazole, Hydrochloride
      DescriptionA potent, cell-permeable, and selective inhibitor of COX-1 (IC50 = 28 nM; human recombinant COX-1). Does not significantly inhibit COX-2 (IC50 = 65 µM, human recombinant COX-2). Reported to be orally active and displays analgesic properties in chemical nociceptive animal models. Also reported to exhibit anti-inflammatory effects and suppress prostaglandin E2 and thromboxane 2 levels in collagen-induced arthritis in rats. Shown to be 100 times more potent than aspirin in inhibiting arachidonic acid- and collagen-induced human and guinea pig platelet aggregation.
      FormPale yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number130717-51-0
      Chemical formulaC₂₃H₂₅N₃O₃S • HCl
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (5 mg/ml), H₂O (4 mg/ml), or 1 N HCl (2 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Hygroscopic
      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
      ReferencesOchi, T., and Goto, T. 2002. Br. J. Pharmacol. 135, 782.
      Ochi, T., et al. 2000. Eur. J. Pharmacol. 391, 49.
      Tanaka, A., et al. 1994. J. Med. Chem. 37, 1189.
      Dohi, M., et al. 1993. Eur. J. Pharmacol. 243, 179.