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

Overview

Replacement Information

Key Specifications Table

Empirical FormulaCAS #
C₂₃H₂₆F₂N₂O₄ 208255-80-5

Pricing & Availability

Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
565770-10MG
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      Plastic ampoule 10 mg
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      565770-5MG
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          Glass bottle 5 mg
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          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

          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 -20°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 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.