MAO-B-IN-5

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

Signaling Pathways >> Neuronal Signaling >> Monoamine Oxidase

Research Areas >> Neurological Disease

MAO-B:34.190 μM (IC50)

MAO-A:0.204 μM (IC50)

MAO-B-IN-5 (compound D0) (Sf9 cells) shows inhibitory activities towards MAO with the IC50s of 34.190 µM and 0.204 µM for MAO-A and MAO-B, respectively[1].

MAO-B-IN-5 (1 mg/kg, i.v.; 5 mg/kg, p.o.) shows oral bioavailability in rats (F=13.6%)[1]. Pharmacokinetic Parameters of MAO-B-IN-5 in SD rats[1]. Compound Route Dose (mg/kg) Cmax (ng/mL) AUCt (ng·h/mL) T1/2 (h) Vss (h) Cl (mL/min/kg) F (%) D0 iv 1 809 347 0.37 1.11 47.1 / po 5 163 284 1.27 / / 16.3SD rats; 1 mg/kg, i.v.; 5 mg/kg, p.o.[1]. Animal Model: SD rats[1] Dosage: 1, 5 mg/kg Administration: 1 mg/kg, i.v.; 5 mg/kg, p.o. Result: Showed oral bioavailability in rats (F=16.3%).

[1]. Wang Z,et al. Enhancing monoamine oxidase B inhibitory activity via chiral fluorination: Structure-activity relationship, biological evaluation, and molecular docking study. Eur J Med Chem. 2022; 228:114025.