MAO-B-IN-61

MAO-B-IN-61 (PBC21) exhibits potent and highly selective MAO-B inhibitory activity, with an IC₅₀ value of 14 nM and a selectivity index (SI) > 2857 against MAO-A^[1].
MAO-B-IN-61 (7-28 nM) is a mixed-type MAO-B inhibitor; determination via Lineweaver-Burk analysis using five different concentrations of the substrate benzylamine yielded a Ki value of 6.0 nM^[1].
MAO-B-IN-61 (28 nM; 30-minute pre-incubation, 6-hour dialysis) is a reversible MAO-B inhibitor; following dialysis, enzyme activity recovered from 41.28% (non-dialyzed) to 82.59%, consistent with results observed for the reversible control drug Safinamide (HY-70057)^[1].
MAO-B-IN-61 (40 µM) shows weak inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with residual activities of 21.86% and 79.67%, respectively (IC₅₀ > 40 µM for both), indicating significantly higher selectivity for MAO-B than for cholinesterases^[1].
MAO-B-IN-61 (0-30 µM; 24 h) exhibits no significant cytotoxicity toward SH-SY5Y, HepG2, and HK-2 cells, with cell viability remaining above 70% at concentrations up to 30 μM^[1].
MAO-B-IN-61 demonstrates favorable metabolic stability in rat and human liver microsomes; over a 30-minute incubation period, the half-life (t_1/2) values are 5.60 min (CLint = 246 µL/min/mg protein) and 14.15 min (CLint = 98 µL/min/mg protein), respectively^[1].
MAO-B-IN-61 is predicted to possess good oral bioavailability and blood-brain barrier permeability by in silico simulations using the Deep-PK server^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.