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DAPT(GSI-IX)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
DAPT(GSI-IX)图片
CAS NO:208255-80-5
规格:98%
分子量:432.46
包装与价格:
包装价格(元)
10mg电议
50mg电议
500mg电议

产品介绍
γ-secretase inhibitor,potent and specific
CAS:208255-80-5
分子式:C23H26F2N2O4
分子量:432.46
纯度:98%
存储:Store at -20°C

Background:

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 levelsin vivoin 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