TAK-070 (TAK070) is a selective, nonpeptidic, noncompetitive BACE1 inhibitor with IC50 of 3.15 uM in cell-free assays.
TAK-070 suppresses the secretion of Aβ with minimum effective concentrations (MECs) for Aβ40 and Aβ42 of 100 and 1000 nM respectively in human IMR-32 neuroblastoma cells.
TAK-070 also stimulates sAPPα production with MEC of 100 nM.
TAK-070 significantly decreases the secreted level of both human Swedish sAPPβ and mouse endogenous sAPPβ, N-terminal counterparts of APP generated by BACE1 cleavage, by ∼16 and ∼19% respectively at 3 uM.
TAK-070 ameliorates Abeta pathology and behavioral deficits in a mouse model of Alzheimer's disease.
