Potent, selective inhibitor of O-GlcNAcase (Ki = 21 nM for human O-GlcNAcase). Increases levels of O-GlcNAc-modified proteins in cellular assays and in vivo. Suppresses phosphorylation of tau protein in rat cortex and hippocampus.1 Stabilizes tau against aggregation and slows neurodegeneration.2 Prevents cognitive decline and amyloid plaque formation in bigenic tau/APP mutant mice.3 Active in vivo and blood brain barrier permeable.
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