MAO-B-IN-5 is a potent, selective, and orally active MAO-B inhibitor with an IC50 of 0.204 μM, showing potential for research in Parkinson's disease (PD) [1].

MAO-B:34.190 μM, MAO-A:0.204 μM

MAO-B-IN-5 (compound D0) exhibits inhibitory activity against MAO, with IC50 values of 34.190 μM for MAO-A and 0.204 μM for MAO-B in Sf9 cells [1].

MAO-B-IN-5 demonstrates oral bioavailability (F=13.6%) in rats when administered at doses of 1 mg/kg intravenously (i.v.) and 5 mg/kg orally (p.o.). The pharmacokinetic profile of MAO-B-IN-5 in Sprague-Dawley (SD) rats is detailed, with the compound showing a maximum concentration (Cmax) of 809 ng/mL and an area under the curve (AUC) of 347 ng·h/mL following a 1 mg/kg intravenous dose; the half-life (T1/2) is 0.37 hours, volume of steady state (Vss) is 1.11 h, and clearance (Cl) is 47.1 mL/min/kg. Orally administered at a dose of 5 mg/kg, MAO-B-IN-5 has a Cmax of 163 ng/mL, an AUC of 284 ng·h/mL, and a T1/2 of 1.27 hours, with an oral bioavailability of 16.3%.