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

236005
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₃H₂₅N₃O₃S • HCl 130717-51-0

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      236005-5MG
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          Plastic ampoule 5 mg
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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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          236005

          References

          Reference overview
          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.
          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.

          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 +2°C to +8°C
          Hygroscopic
          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
          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.