511071 PAF Receptor Antagonist, ABT-491 - CAS 189689-94-9 - Calbiochem

511071
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₈H₂₂FN₅O₂ • HCl 189689-94-9

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      511071-2MG
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          Plastic ampoule 2 mg
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          Description
          OverviewAn orally available ethynylindole compound that potently inhibits PAF (platelet-activating factor) binding to its receptor in a competitive manner in equilibrium binding studies (Ki = 0.6 or 3.8 nM, respectively, using intact human platelets or isolated rabbit platelet membrane; [PAF] = 0.6 nM), while a non-competitive inhibition is observed if the membrane-bound receptors are pre-incubated with the antagonist prior to the addition of PAF, presumably due to a slower antagonist dissociation rate. Shown to effectively antagonize PAF-induced platelet and neutrophil responses at submicromolar concentrations in vitro and exhibit in vivo efficacy in alleviating PAF-mediated inflammatory and pathological processes in various animals, including guinea pigs, mice, and rats, via either i.v. or p.o.. Reported to display high specificity toward PAF receptor as evaluated in binding assays employing a wide variety of receptors and ion channels.
          Catalogue Number511071
          Brand Family Calbiochem®
          Synonyms1-(N,N-Dimethylcarbamoyl)-4-ethynyl-3-(3-fluoro-4-((1H-2-methylimidazo[4,5-c]pyridin-1-yl)methyl)benzoyl)-indole, HCl
          References
          ReferencesCurtin, M.L., et al. 1998. J. Med. Chem. 41, 74.
          Albert, D.H., et al. 1998. J. Pharmacol. Exp. Ther. 284, 83.
          Albert, D.H., et al. 1997. Eur. J. Pharmacol. 325, 69.
          Product Information
          CAS number189689-94-9
          FormOff-white solid
          Hill FormulaC₂₈H₂₂FN₅O₂ • HCl
          Chemical formulaC₂₈H₂₂FN₅O₂ • HCl
          Hygroscopic Hygroscopic
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Purity≥98% by HPLC
          Physicochemical Information
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          S PhraseS: 22-24/25

          Do not breathe dust.
          Avoid contact with skin and eyes.
          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 3 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
          511071

          References

          Reference overview
          Curtin, M.L., et al. 1998. J. Med. Chem. 41, 74.
          Albert, D.H., et al. 1998. J. Pharmacol. Exp. Ther. 284, 83.
          Albert, D.H., et al. 1997. Eur. J. Pharmacol. 325, 69.
          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.

          Revision28-October-2009 RFH
          Synonyms1-(N,N-Dimethylcarbamoyl)-4-ethynyl-3-(3-fluoro-4-((1H-2-methylimidazo[4,5-c]pyridin-1-yl)methyl)benzoyl)-indole, HCl
          DescriptionAn orally available ethynylindole compound that potently inhibits PAF (platelet-activating factor) binding to its receptor in a competitive manner in equilibrium binding studies (Ki = 0.6 or 3.8 nM, respectively, using intact human platelets or isolated rabbit platelet membrane; [PAF] = 0.6 nM), while a non-competitive inhibition is observed if the membrane-bound receptors are pre-incubated with the antagonist prior to the addition of PAF, presumably due to a slower antagonist dissociation rate. Shown to effectively antagonize PAF-induced platelet and neutrophil responses at submicromolar concentrations in vitro and exhibit in vivo efficacy in alleviating PAF-mediated inflammatory and pathological processes in various animals, including guinea pigs, mice, and rats, via either i.v. or p.o.. Reported to display high specificity toward PAF receptor as evaluated in binding assays employing a wide variety of receptors and ion channels.
          FormOff-white solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number189689-94-9
          Chemical formulaC₂₈H₂₂FN₅O₂ • HCl
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityH₂O (10 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 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesCurtin, M.L., et al. 1998. J. Med. Chem. 41, 74.
          Albert, D.H., et al. 1998. J. Pharmacol. Exp. Ther. 284, 83.
          Albert, D.H., et al. 1997. Eur. J. Pharmacol. 325, 69.