產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 10mg 50mg 500mg
CAS	208255-80-5
別名	gamma-Secretase Inhibitor IX, DAPT, GSI-IX
化學(xué)名	tert-butyl (2S)-2-[[(2S)-2-[[2-(3,5-difluorophenyl)acetyl]amino]propanoyl]amino]-2-phenylacetate
分子式	C23H26F2N2O4
分子量	432.46
溶解度	≥ 21.623mg/mL in DMSO, ≥ 16.36 mg/mL in EtOH with ultrasonic
儲存條件	Store at 4°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

DAPT, N-[N-(3,5-Difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl Ester, is a potent and specific inhibitor of γ-secretase, a multimeric membrane protein complex that catalyzes proteolytic cleavage of amyloid precursor protein (APP) resulting in the accumulation of amyloi-β (Aβ) peptides which is associated with early on-set of familial Alzheimer’s disease (AD). It directly binds to the C-terminal fragment of the catalytic center of γ-secretase, presenilin (PS), especially within the transmenbrane domain 7 or more C-terminal region, resulting in the synthesis of a photoactivable DAPT derivative. Through oral administration, DAPT dose-dependently reduced Aβ peptides levels in vivo in Plasma and cerebrospinal fluid in young (6 months old, plaque-free) and aged (17 months old, plaque-bearing) Tg2576 mice.

Reference

[1].Thomas A. Lanz, Carol S. Himes, Giovanni Pallante, Lisa Adams, Shinji Yamazaki, Ben Amore, and Kalpana M. Merchant. The γ-secretase inhibitor N-[N-(3,5-Difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl Ester reduces Aβ levels in vivo in plasma and cerebrospinal fluid in young (plague-free) and aged (plaque-bearing) Tg2576 mice. The Journal of Pharmacology and Experimental Therapeutics 2003: 305 (3) 864-871

[2].Yuichi Morohashi, Toshiyuki Kan, Yusuke Tominari, Haruhiko Fuwa, Yumiko Okamura, Naoto Watanabe, Chihiro Sato, Hideaki Natsugari, Tohru Fukuyama, Takeshi Iwatsubo, and Taisuke Tomita. C-terminal fragment of presenilin is the molecular target of a dipeptidic γ-secretase-specific inhibitor DAPT (N-[N-(3,5-Difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl Ester). The Journal of Biological Chemistry 2006: 281(21) 14670-14676

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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