Luvadaxistat (TAK-831, NBI-1065844) is a highly potent, selective D-amino acid oxidase (DAAO) inhibitor with IC50 of 14 nM against human recombinant DAAO enzyme.
TAK-831 (Luvadaxistat) inhibits the formation of H2O2, the co-product of D-serine catalysis, with an IC50 of 12 nM, in a cellular assay using CHO cells expressing recombinant human DAAO.
TAK-831 (Luvadaxistat) inhibits H2O2 formation with IC50 of 5.1 nM in CHO cells expressing recombinant mouse DAAO.
TAK-831 (Luvadaxistat) shows very little off-target activity when profiled in a comprehensive selectivity panel of enzyme and radioactivity binding.
TAK-831 (Luvadaxistat) caused a dose- and exposure-dependent blockade of PGM019260 binding in the cerebellum with ED50 of 0.93 mg/kg in enzyme occupancy studies in mice.
TAK-831 (Luvadaxistat) (3 mg/kg p.o.) significantly reverses a poly(I:C)-induced deficit, improves social behavior in the SI test in BALB/c animals.