NB-533 is an orally active and brain-penetrant BACE-1 inhibitor with a human IC 50 of 0.002 μM. NB-533 also inhibits human cathepsin D with an IC 50 of 0.001 μM. NB-533 inhibits amyloidogenic amyloid precursor protein (APP) processing and reduces Aβ 40 release. NB-533 reduces brain levels of APP metabolite C99 and Aβ 40 in transgenic mice. NB-533 can be used for the research of Alzheimer’s disease.
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