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565793 γ-Secretase Inhibitor XXIV, BMS299897 - CAS 290315-45-6 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical FormulaCAS #
C₂₄H₂₁ClF₃NO₄S 290315-45-6

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565793-5MG
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      Glass bottle 5 mg
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      Description
      OverviewA cell-permeable sulfonamide compound that preferentially inhibits cellular γ-secretase cleavage of APP CTF over Notch-1 (IC50 = 7.1 and 105.9 nM, respectively) in a presenillin 1-/PS1-selective manner (IC50 = 8 and 308 nM against PS1 and PS2, respectively). BMS-299897 is shown to be orally available, readily cross blood-brain-barrier (<15 min), and effectively suppress plasma and brain Aβ level in human APP-bearing transgenic mice in a time- and dose-dependent manner (optimal p.o. dose 100 mg/kg) in vivo.
      Catalogue Number565793
      Brand Family Calbiochem®
      SynonymsBMS-299897, BMS 299897, 4-(2-((1R)-1-(((4-Chlorophenyl)sulfonyl)-2,5-difluoroanilino)ethyl)-5-fluorophenyl)butanoic acid
      References
      ReferencesZhao, B., et al. 2008. J. Biol. Chem. 283, 2927.
      Barten, D.M., et al. 2005. J. Pharmacol. Exp. Ther. 312, 635.
      Anderson, J.J., et al. 2005. Biochem. Pharmacol. 69, 689.
      Product Information
      CAS number290315-45-6
      FormWhite solid
      Hill FormulaC₂₄H₂₁ClF₃NO₄S
      Chemical formulaC₂₄H₂₁ClF₃NO₄S
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥97% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      γ-Secretase Inhibitor XXIV, BMS299897 - CAS 290315-45-6 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      γ-Secretase Inhibitor XXIV, BMS299897 - CAS 290315-45-6 - Calbiochem Certificates of Analysis

      TitleLot Number
      565793

      References

      Reference overview
      Zhao, B., et al. 2008. J. Biol. Chem. 283, 2927.
      Barten, D.M., et al. 2005. J. Pharmacol. Exp. Ther. 312, 635.
      Anderson, J.J., et al. 2005. Biochem. Pharmacol. 69, 689.
      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.

      Revision16-April-2012 JSW
      SynonymsBMS-299897, BMS 299897, 4-(2-((1R)-1-(((4-Chlorophenyl)sulfonyl)-2,5-difluoroanilino)ethyl)-5-fluorophenyl)butanoic acid
      DescriptionA cell-permeable sulfonamide compound that preferentially inhibits γ-secretase activity toward APP CTF over Notch-1 (IC50 against APPSW CTF and murine ΔE-Notch processing = 7.1 and 105.9 nM, respectively, in HEK293) in a presenillin 1-/PS1-selective manner (IC50 = 8 and 308 nM against APPSW processing in PS1-/-PS2-/-MEF expressing human PS1 and PS2, respectively). BMS-299897 is shown to be orally available, readily cross blood-brain-barrier (<15 min), and effectively suppress plasma and brain Aβ level in transgenic mice bearing normal human APP (APP-YAC) or APPSW/APPK670N/M671L (Tg2576) in a time- and dose-dependent manner (optimal p.o. dose 100 mg/kg) in vivo. However, BMS-299897 is not effective in reducing Aβ in aged, plaque-bearing murine brain and long-term daily drug dosing is reported to result in increased drug metabolizing activity in mice.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number290315-45-6
      Chemical formulaC₂₄H₂₁ClF₃NO₄S
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (50 mg/ml) Ethanol (100 mM)
      Storage +2°C to +8°C
      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
      ReferencesZhao, B., et al. 2008. J. Biol. Chem. 283, 2927.
      Barten, D.M., et al. 2005. J. Pharmacol. Exp. Ther. 312, 635.
      Anderson, J.J., et al. 2005. Biochem. Pharmacol. 69, 689.