TB5 is a potent and selective monoamine oxidase B (MAO-B) inhibitor with Ki values of 110 and 1,450 nM for MAO-B and MAO-A, respectively.1 It interacts with the catalytic site of human MAO-B in a competitive manner. In an enzyme assay, MAO-B activity increases?from 37% to 97% following inhibitor washout, indicating TB5 binding is reversible.?TB5 also demonstrates permeability in a parallel artificial membrane permeation assay (PAMPA), a model for the blood-brain barrier, and has minimal cytotoxicity (>84% cell viability) in HepG2 cells at a concentrations up to 25 μM.
1.Mathew, B., Haridas, A., U?ar, G., et al.Synthesis, biochemistry, and computational studies of brominated thienyl chalcones: A new class of reversible MAO-B inhibitorsChemMedChem11(11)1161-1171(2016)
















