产品
编 号：F751684
分子式：C19H20F2N2O2
分子量：346.37
分子式：C19H20F2N2O2
分子量：346.37
产品类型
规格
价格
是否有货
结构图
CAS No: 2376198-66-0
产品详情
生物活性：
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).
体内研究：
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%).MAO-B-IN-6 (0.08, 0.4, 2 mg/kg; i.p.) diaplays stronger MAO-B inhibitory activity.MAO-B-IN-6 (0.625, 1.25, 2.5 mg/kg; i.p.) increases the rearing activity in a dose-dependent manner.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.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.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.Pharmacokinetic Parameters of MAO-B-IN-6 in SD rats and cynomolgus monkeys.CompoundRoute Dose (mg/kg) Cmax (ng/mL)AUCt (ng·h/mL)T1/2 (h)Vss (h)Cl (mL/min/kg)F (%)
D5 (Rats)iv16905050.671.3732.9/
D5 (Rats)po5100014000.57//55.2
D5 (Monkeys)iv192421201.771.067.54/
D5 (Monkeys)po5228011,3002.80//107.1
SD rats; 1 mg/kg, i.v.; 5 mg/kg, p.o.; Cynomolgus monkeys; 1 mg/kg, i.v.; 5 mg/kg, p.o..Animal Model:SD rats
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
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
Dosage:0.08, 0.4, 2 mg/kg
Administration:i.p.
Result:Displayed stronger MAO-B inhibitory activity.
Animal Model:PD mouse mode
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
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
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.
体外研究：
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.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).MAO-B-IN-6 (10 μM) shows high permeability through MDR1-MDCK II cell monolayers.
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).
体内研究：
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%).MAO-B-IN-6 (0.08, 0.4, 2 mg/kg; i.p.) diaplays stronger MAO-B inhibitory activity.MAO-B-IN-6 (0.625, 1.25, 2.5 mg/kg; i.p.) increases the rearing activity in a dose-dependent manner.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.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.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.Pharmacokinetic Parameters of MAO-B-IN-6 in SD rats and cynomolgus monkeys.CompoundRoute Dose (mg/kg) Cmax (ng/mL)AUCt (ng·h/mL)T1/2 (h)Vss (h)Cl (mL/min/kg)F (%)
D5 (Rats)iv16905050.671.3732.9/
D5 (Rats)po5100014000.57//55.2
D5 (Monkeys)iv192421201.771.067.54/
D5 (Monkeys)po5228011,3002.80//107.1
SD rats; 1 mg/kg, i.v.; 5 mg/kg, p.o.; Cynomolgus monkeys; 1 mg/kg, i.v.; 5 mg/kg, p.o..Animal Model:SD rats
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
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
Dosage:0.08, 0.4, 2 mg/kg
Administration:i.p.
Result:Displayed stronger MAO-B inhibitory activity.
Animal Model:PD mouse mode
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
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
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.
体外研究：
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.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).MAO-B-IN-6 (10 μM) shows high permeability through MDR1-MDCK II cell monolayers.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备