565770

DAPT

≥98% (HPLC), lyophilized, γ-secretase inhibitor, Calbiochem^®

• Synonyme(s) : γ-Secretase Inhibitor IX, DAPT, N-[N-(3,5-Difluorophenacetyl-L-alanyl)]-S-phenylglycine t-Butyl Ester
• Formule empirique (notation de Hill): C₂₃H₂₆F₂N₂O₄
• Numéro CAS: 208255-80-5
• Poids moléculaire : 432.46
• Numéro MDL: MFCD04974585
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.28

Propriétés

• product name: γ-Secretase Inhibitor IX, Gamma-Secretase Inhibitor IX - CAS 208255-80-5, is a cell-permeable inhibitor of γ-secretase (Aβtotal IC₅₀ = 115 nM, Aβ42 IC₅₀ = 200 nM).
• Niveau de qualité: 100
• Pureté: ≥98% (HPLC)
• Forme: lyophilized
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Solubilité: DMSO: 20 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: −20°C
• InChI: 1S/C23H26F2N2O4/c1-14(26-19(28)12-15-10-17(24)13-18(25)11-15)21(29)27-20(16-8-6-5-7-9-16)22(30)31-23(2,3)4/h5-11,13-14,20H,12H2,1-4H3,(H,26,28)(H,27,29)/t14-,20-/m0/s1
• Clé InChI: DWJXYEABWRJFSP-XOBRGWDASA-N

Description

Description générale

A 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.

A cell-permeable dipeptide that suppresses Aβ production by blocking γ-secretase (Aβ_total 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.

Actions biochimiques/physiologiques

Cell permeable: yes

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 115 nM suppressing Aβtotal production; 200 nM suppressing Aβ42 production

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Autres remarques

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. Neuron43, 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.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable