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

The PAF Receptor Antagonist, ABT-491, also referenced under CAS 189689-94-9, controls the biological activity of PAF Receptor. This small molecule/inhibitor is primarily used for Membrane applications.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 1-(N,N-Dimethylcarbamoyl)-4-ethynyl-3-(3-fluoro-4-((1H-2-methylimidazo[4,5-c]pyridin-1-yl)methyl)benzoyl)-indole, HCl

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511071
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
189689-94-9C₂₈H₂₂FN₅O₂ • HCl

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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
      Quality LevelMQ100
      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
      Global Trade Item Number
      Catalogue Number GTIN
      511071-2MG 04055977271997

      Documentation

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

      Title

      Safety Data Sheet (SDS) 

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