Discovery of Begacestat, a Notch-1-Sparing γ-Secretase Inhibitor for the Treatment of Alzheimer's Disease (original) (raw)

Discovery of Begacestat, a Notch-1-Sparing γ-Secretase Inhibitor for the Treatment of Alzheimer's Disease

Journal of medicinal …, 2008

Abstract

Not only is 9 a potent GSI but it also has promising Notch-1-sparing selectivity (10-fold). This compound was profiled for in vivo reduction of brain Aβ 40 and Aβ 42 in the Tg2576 mouse model at the 4 h time point when given 100 mg/kg po. Brain Aβ 40 and Aβ 42 in the Tg2576 ...

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