Vafidemstat (ORY-2001, ORY2001) is a potent, selective, brain penetrant dual lysine-specific histone demethylase (LSD1, KDM1A)/MAO-B inhibitor with IC50 of 105 nM (KDM1A) and 58 nM (MAO-B).
ORY-2001 corrects memory deficit and behavior alterations including aggression and social interaction deficits in SAMP8 mice and social avoidance in the rat rearing isolation model.
ORY-2001 increases the responsiveness of IEGs, induces genes required for cognitive function and reduces neuroinflammation in the brain of mouse models of CNS disease.
