Chemical Name: (2R)-2-[[(4-Chlorophenyl)sulfonyl][[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoropentanamide
Biological ActivityHighly potent γ-secretase inhibitor (Aβ40 IC50 = 0.3 nM). Exhibits >137-fold selectivity for amyloid-β precursor protein (APP) processing over Notch. Reduces plasma and brain Aβ40 and Aβ42 levels in vivo. Orally bioavailable.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Discovery and evaluation of BMS-708163, a potent, selective and orally bioavailable γ-secretase inhibitor.
Gillman et al.
ACS Med.Chem.Lett., 2010;1:120
Pharmacodynamics of selective inhibition of γ-secretase by avagacestat.
Albright et al.
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