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Journal: Neurotherapeutics
Article Title: Discovery of an APP-selective BACE1 inhibitor for Alzheimer's disease
doi: 10.1016/j.neurot.2025.e00610
Figure Lengend Snippet: Inhibitory activity and brain permeability of FAH65E(-) . Shown are (A) dose-response curves for FAH65 racemate and the FAH65E(+) and (-) enantiomers in the P5-P5′ assay and (B) sAPPβ and (C) Aβ1-42 in CHO-7W cells after treatment with increasing concentrations of FAH65 racemate and enantiomers. Legend in B also applies to C. Data graphed as the mean and SEM. (D) FAH65E(-) (black line) and sAPP β (blue dashed line) levels in brain from ApoE4TR-5XFAD mice after oral delivery of 30 mg/kg FAH65E(-) doses are shown. PK-PD study design did not include 0 h timepoint untreated mice but included time points 1, 2, 4 and 6 h after last dose on Day 2. N = 3 mice per time point.
Article Snippet: Media was assayed using an AlphaLISA for Aβ1-42 (Perkin Elmer catalog # AL276C),
Techniques: Activity Assay, Permeability