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565770 γ-Secretase Inhibitor IX - CAS 208255-80-5 - Calbiochem

565770
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
208255-80-5C₂₃H₂₆F₂N₂O₄

Products

Catalogue NumberPackaging Qty/Pack
565770-10MG Plastic ampoule 10 mg
565770-5MG Glass bottle 5 mg
Description
OverviewA cell-permeable dipeptide that suppresses Aβ production by blocking γ-secretase (Aβtotal IC50 = 115 nM, Aβ42 IC50 = 200 nM). Prevents Aβ34 generation in murine N2a cells and hAPP/hBACE-1 transfected human HEK 293 cells. Reported to be functionally active in both HEK 293 cells and neuronal cultures without affecting the secretion of amyloid-β precursor protein (APP). Also shown to lower Aβ levels acutely in APP-transgenic mice. Reported to reduce extracellular Aβ plaques and intracellular Aβ accumulation in 3xTgAD transgenic mice. A 25 mM (5 mg/462 µl) solution of γ-Secretase Inhibitor IX (Cat. No. 565784) in DMSO is also available.
Catalogue Number565770
Brand Family Calbiochem®
SynonymsDAPT, N-[N-(3,5-Difluorophenacetyl-L-alanyl)]-S-phenylglycine t-Butyl Ester
References
ReferencesMorohashi, Y., et al. 2006. J. Bio. Chem. Vol. 281, 14670.
Nishitomo, K. et al. 2006 J. Neurochem. 99, 1555.
Oddo, S., et al. 2004. Neuron 43, 321.
Dovey, H.F., et al. 2001. J. Neurochem. 76, 173.
Sastre, M., et al. 2001. EMBO Rep. 2, 835.
Vandermeeren, M., et al. 2001. Neurosci. Lett. 315, 145.
Product Information
CAS number208255-80-5
ATP CompetitiveN
FormLyophilized
Hill FormulaC₂₃H₂₆F₂N₂O₄
Chemical formulaC₂₃H₂₆F₂N₂O₄
ReversibleN
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary Targettotal
Primary Target IC<sub>50</sub>115 nM suppressing Aβtotal production; 200 nM suppressing Aβ42 production
Purity≥98% 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 Ambient Temperature Only
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
565770-10MG 04055977267778
565770-5MG 07790788059941

Documentation

γ-Secretase Inhibitor IX - CAS 208255-80-5 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

γ-Secretase Inhibitor IX - CAS 208255-80-5 - Calbiochem Certificates of Analysis

TitleLot Number
565770

References

Reference overview
Morohashi, Y., et al. 2006. J. Bio. Chem. Vol. 281, 14670.
Nishitomo, K. et al. 2006 J. Neurochem. 99, 1555.
Oddo, S., et al. 2004. Neuron 43, 321.
Dovey, H.F., et al. 2001. J. Neurochem. 76, 173.
Sastre, M., et al. 2001. EMBO Rep. 2, 835.
Vandermeeren, M., et al. 2001. Neurosci. Lett. 315, 145.

Citations

Title
  • Yunzhou Dong, et al. (2006) Calpain inhibitor MDL28170 modulates Aβ formation by inhibiting the formation of intermediate Aβ46 and protecting Aβ from degradation. FASEB Journal in press,.
  • Aurelie Olivier, et al. (2005) The Notch ligand delta-1 is a hematopoietic development co- factor for plasmacytoid dendritic cells. Blood 107, 2694-2701.
  • 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.

    Revision12-November-2007 JSW
    SynonymsDAPT, N-[N-(3,5-Difluorophenacetyl-L-alanyl)]-S-phenylglycine t-Butyl Ester
    DescriptionA cell-permeable dipeptide that inhibits γ-secretase activity and suppresses Aβ production (Aβ total IC50 = 115 nM; Aβ42 IC50 = 200 nM). Reported to be functionally active in both HEK293 cells overexpressing human APP751 and neuronal cultures, however, it does not affect the secretion of amyloid-b precursor protein (APP). Effective in acutely lowering Ab in APPV717F-transgenic mice. Also effective in inhibiting the production of an ~6 kDa C-terminal cleavage product (CTFg) in HEK293 cells stably transfected with the Swedish mutant, βAPP695. Reported to reduce extracellular Aβ plaques and intracellular Aβ accumulation in 3xTgAD transgenic mice.
    FormLyophilized
    Intert gas (Yes/No) Packaged under inert gas
    CAS number208255-80-5
    Chemical formulaC₂₃H₂₆F₂N₂O₄
    Structure formulaStructure formula
    Purity≥98% by HPLC
    SolubilityDMSO (20 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
    ReferencesMorohashi, Y., et al. 2006. J. Bio. Chem. Vol. 281, 14670.
    Nishitomo, K. et al. 2006 J. Neurochem. 99, 1555.
    Oddo, S., et al. 2004. Neuron 43, 321.
    Dovey, H.F., et al. 2001. J. Neurochem. 76, 173.
    Sastre, M., et al. 2001. EMBO Rep. 2, 835.
    Vandermeeren, M., et al. 2001. Neurosci. Lett. 315, 145.
    Citation
  • Yunzhou Dong, et al. (2006) Calpain inhibitor MDL28170 modulates Aβ formation by inhibiting the formation of intermediate Aβ46 and protecting Aβ from degradation. FASEB Journal in press,.
  • Aurelie Olivier, et al. (2005) The Notch ligand delta-1 is a hematopoietic development co- factor for plasmacytoid dendritic cells. Blood 107, 2694-2701.