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565789 γ-Secretase Inhibitor XX - CAS 209984-56-5 - Calbiochem

This γ-secretase inhibitor, CAS 209984-56-5, is a cell-permeable dibenzazepine compound that lowers both brain and plasma Aβ40 levels by ~72% in Tg2576 mutant APP transgenic mouse model.

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

Synonyms: (S,S)-2-[2-(3,5-Difluorophenyl)acetylamino]-N-(5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)propionamide, DBZ, Dibenzazepine

Primary Target: γ-secretase
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565789
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
209984-56-5C₂₆H₂₃F₂N₃O₃

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      Description
      OverviewA cell-permeable dibenzazepine (dbz) compound that acts as a potent γ-secretase inhibitor and significantly lowers both brain and plasma Aβ40 levels by ~72% in Tg2576 mutant APP transgenic mouse model (100 µmol/kg, b.i.d). Induces a heterogeneous reorganization of the crypt structural-proliferative units in the intestinal tract and of the stem cell niche in the colon. Also potently inhibits Notch processing (IC50 = 1.7 nM in SupT1 cells) and induces conversion of proliferative crypt cells to post-mitotic goblet cells in both the C57BL/6 and ApcMin mouse models (10 µmol/kg, i.p).
      Catalogue Number565789
      Brand Family Calbiochem®
      Synonyms(S,S)-2-[2-(3,5-Difluorophenyl)acetylamino]-N-(5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)propionamide, DBZ, Dibenzazepine
      References
      ReferencesDroy-Dupré, L., et al. 2012. Dis. Model Mech. 5, 107.
      van Es, J.H., et al. 2005. Nature 435, 959.
      Milano, J., et al. 2004. Toxicol. Sci. 82, 341.
      Product Information
      CAS number209984-56-5
      ATP CompetitiveN
      FormWhite solid
      Hill FormulaC₂₆H₂₃F₂N₃O₃
      Chemical formulaC₂₆H₂₃F₂N₃O₃
      ReversibleN
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary Targetγ-secretase
      Primary Target IC<sub>50</sub>1.7 nM inhibiting Notch processing in SupT1 cells
      Purity≥95% 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage -20°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 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
      565789-1MG 04055977191837

      Documentation

      γ-Secretase Inhibitor XX - CAS 209984-56-5 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      γ-Secretase Inhibitor XX - CAS 209984-56-5 - Calbiochem Certificates of Analysis

      TitleLot Number
      565789

      References

      Reference overview
      Droy-Dupré, L., et al. 2012. Dis. Model Mech. 5, 107.
      van Es, J.H., et al. 2005. Nature 435, 959.
      Milano, J., et al. 2004. Toxicol. Sci. 82, 341.

      Citations

      Title
    • Droy-Dupré, L., et al. 2012. Dis. Model Mech. 5, 107.
      		•
      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-February-2012 RFH
      Synonyms(S,S)-2-[2-(3,5-Difluorophenyl)acetylamino]-N-(5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)propionamide, DBZ, Dibenzazepine
      DescriptionA cell-permeable, potent γ-secretase inhibitor that significantly lowers both brain and plasma Aβ40 levels by ~72% in Tg2576 mutant APP transgenic mouse model (100 µmol/kg, b.i.d). Induces a heterogeneous reorganization of the crypt structural-proliferative units in the intestinal tract and of the stem cell niche in the colon. Also potently inhibits Notch processing (IC50 = 1.7 nM in SupT1 cells) and induces conversion of proliferative crypt cells to post-mitotic goblet cells in both the C57BL/6 and ApcMin mouse models (10 µmol/kg, i.p).
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number209984-56-5
      Chemical formulaC₂₆H₂₃F₂N₃O₃
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (10 mg/ml)
      Storage Protect from light
      -20°C
      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
      ReferencesDroy-Dupré, L., et al. 2012. Dis. Model Mech. 5, 107.
      van Es, J.H., et al. 2005. Nature 435, 959.
      Milano, J., et al. 2004. Toxicol. Sci. 82, 341.
      Citation
    • Droy-Dupré, L., et al. 2012. Dis. Model Mech. 5, 107.
      		•