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MAO-B-IN-6
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MAO-B-IN-6图片
CAS NO:2376198-66-0
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
MAO-B-IN-6 是一种有效的、选择性和具有口服活性的MAO-B抑制剂,IC50值为 0.019 μM。MAO-B-IN-6 在体外和体内均显示比 Safinamide 更有效。MAO-B-IN-6 具有研究帕金森病 (PD) 的潜力。
生物活性

MAO-B-IN-6 is a potent, selective and orally activeMAO-Binhibitor with anIC50of 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].

IC50& Target[1]

MAO-B

0.019 μM (IC50)

MAO-A

46.365 μM (IC50)

体外研究
(In Vitro)

MAO-B-IN-6 (compound D5) (Sf9 cells) shows inhibitory activities towards monoamine oxidase (MAO) with theIC50s 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].

体内研究
(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].

CompoundRouteDose (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.[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.
分子量

346.37

Formula

C19H20F2N2O2

CAS 号

2376198-66-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.