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.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
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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