Chemical Name: (2S)-2-Hydroxy-3-methyl-N-[(1S)-1-methyl-2-oxo-2-[[(1S)-2,3,4,5-tetrahydro-3-methyl-2-oxo-1H-3-benzazepin-1-yl]amino]ethyl]butanamide
Biological Activityγ-secretase pseudo-inhibitor. Inhibits Aβ secretion from cells in vitro and increases accumulation of γ-secretase products and long Aβ species in vitro and in vivo. Also attenuates the accumulation of activated microglia and neurological injury in a traumatic brain injury animal model.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Development of semagacestat (LY450139), a functional gamma-secretase inhibitor, for the treatment of Alzheimer's disease.
Henley et al.
Expert Opin.Pharmacother., 2009;10:1657
Concentration-dependent modulation of amyloid-beta in vivo and in vitro using the gamma-secretase inhibitor, LY-450139.
Lanz et al.
Semagacestat is a pseudo-inhibitor of γ-secretase.
Tagami et al.
Cell Rep., 2017;21:259
Gamma-secretase inhibitors attenuate neurotrauma and neurogenic acute lung injury in rats by rescuing the accumulation of hypertrophic microglia.
Lin et al.
Cell Physiol.Biochem., 2017;44:1726
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