Bioactivity | MAO-B-IN-6 is a potent, selective and orally active MAO-B inhibitor with an IC50 of 0.019 µM. MAO-B-IN-6 shows more efficacious than Safinamide in vitro and in vivo. MAO-B-IN-6 has the potential for the research of parkinson's disease (PD)[1]. |
Invitro | MAO-B-IN-6 (compound D5) (Sf9 cells) shows inhibitory activities towards monoamine oxidase (MAO) with the IC50s of 46.365 µM and 0.019 µM for MAO-A and MAO-B, respectively[1].MAO-B-IN-6 shows no inhibition potential towards cytochrome P450 (IC50=>29 µM for 1A2, 2B6, 2C8, 2C9, 2C19, 2D6 and 3A4/5 enzymes)[1].MAO-B-IN-6 (10 µM) shows high permeability through MDR1-MDCK II cell monolayers[1]. |
In Vivo | MAO-B-IN-6 (1 mg/kg, i.v.; 5 mg/kg, p.o.) shows oral bioavailability in rats (F=55.2%) and monkeys (F=107.1%)[1].MAO-B-IN-6 (0.08, 0.4, 2 mg/kg; i.p.) diaplays stronger MAO-B inhibitory activity[1].MAO-B-IN-6 (0.625, 1.25, 2.5 mg/kg; i.p.) increases the rearing activity in a dose-dependent manner[1].MAO-B-IN-6 (0.625, 1.25, 2.5 mg/kg; i.p.) shows a potential efficacy for alleviating dopamine (DA) deficits in the MPTP-induced Parkinson's disease (PD) mouse model[1].MAO-B-IN-6 (0.156, 0.312, 0.625, 1.25 mg/kg; i.p.) increases the effect of levodopa on dopamine concentration in the striatum[1].MAO-B-IN-6 (0.156, 0.312, 0.625, 1.25 mg/kg; i.p.) shows a significant reduction in galantamine-induced tremulous jaw movements[1].Pharmacokinetic Parameters of MAO-B-IN-6 in SD rats and cynomolgus monkeys[1]. Compound |
Name | MAO-B-IN-6 |
CAS | 2376198-66-0 |
Formula | C19H20F2N2O2 |
Molar Mass | 346.37 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |