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

565793
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₄H₂₁ClF₃NO₄S 290315-45-6

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      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®
          Synonyms4-(2-((1R)-1-(((4-Chlorophenyl)sulfonyl)-2,5-difluoroanilino)ethyl)-5-fluorophenyl)butanoic acid , BMS-299897, BMS 299897
          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
          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
          Synonyms4-(2-((1R)-1-(((4-Chlorophenyl)sulfonyl)-2,5-difluoroanilino)ethyl)-5-fluorophenyl)butanoic acid , BMS-299897, BMS 299897
          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.