565770

DAPT

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

• 別名: γ-Secretase Inhibitor IX, DAPT, N-[N-(3,5-Difluorophenacetyl-L-alanyl)]-S-phenylglycine t-Butyl Ester
• 実験式（ヒル表記法）: C₂₃H₂₆F₂N₂O₄
• CAS番号: 208255-80-5
• 分子量: 432.46
• MDL番号: MFCD04974585
• UNSPSCコード: 12352200
• NACRES: NA.28

特性

• 製品名: 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).
• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• フォーム: lyophilized
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 溶解性: DMSO: 20 mg/mL
• 輸送温度: ambient
• 保管温度: −20°C
• SMILES記法: Fc1cc(cc(c1)CC(=O)N[C@@H](C)C(=O)N[C@@H](c2ccccc2)C(=O)OC(C)(C)C)F
• 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
• InChI Key: DWJXYEABWRJFSP-XOBRGWDASA-N

詳細

詳細

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.

生物化学的／生理学的作用

Cell permeable: yes

Product does not compete with ATP.

Reversible: no

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

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

その他情報

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.

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable