2376198-66-0
2376198-66-0 structure
- Name: MAO-B-IN-6
- Chemical Name: MAO-B-IN-6
- CAS Number: 2376198-66-0
- Molecular Formula: C19H20F2N2O2
- Molecular Weight: 346.37
- Catalog: Signaling Pathways Neuronal Signaling Monoamine Oxidase
- Create Date: 2022-09-16 22:38:40
- Modify Date: 2024-01-16 08:17:28
-
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].
| Name | MAO-B-IN-6 |
|---|
| Description | 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]. |
|---|---|
| Related Catalog | |
| Target |
MAO-B:0.019 μM (IC50) MAO-A:46.365 μM (IC50) |
| In Vitro | 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 Route Dose (mg/kg) Cmax (ng/mL) AUCt (ng·h/mL) T1/2 (h) Vss (h) Cl (mL/min/kg) F (%) D5 (Rats) iv 1 690 505 0.67 1.37 32.9 / D5 (Rats) po 5 1000 1400 0.57 / / 55.2 D5 (Monkeys) iv 1 924 2120 1.77 1.06 7.54 / D5 (Monkeys) po 5 2280 11,300 2.80 / / 107.1SD rats; 1 mg/kg, i.v.; 5 mg/kg, p.o.; Cynomolgus monkeys; 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=55.2%). Animal Model: cynomolgus monkeys[1] Dosage: 1, 5 mg/kg Administration: 1 mg/kg, i.v.; 5 mg/kg, p.o. Result: Showed oral bioavailability in monkeys (F=107.1%). Animal Model: mice[1] Dosage: 0.08, 0.4, 2 mg/kg Administration: i.p. Result: Displayed stronger MAO-B inhibitory activity. Animal Model: PD mouse mode[1] Dosage: 0.625, 1.25, 2.5 mg/kg Administration: i.p. Result: Increased the rearing activity in a dose-dependent manner. Animal Model: C57BL/6 mice[1] Dosage: 0.156, 0.312, 0.625, 1.25 mg/kg Administration: i.p. Result: Increased the effect of levodopa on dopamine concentration in the striatum. Animal Model: SD rats[1] Dosage: 0.156, 0.312, 0.625, 1.25 (3.0 mg/kg galantamine, i.p.) Administration: i.p. Result: Showed a significant reduction in galantamine-induced tremulous jaw movements. |
| References |
| Molecular Formula | C19H20F2N2O2 |
|---|---|
| Molecular Weight | 346.37 |