2. Neuronal Signaling
  3. Monoamine Oxidase
  4. MAO-B-IN-6

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。

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MAO-B-IN-6 Chemical Structure

MAO-B-IN-6 Chemical Structure

CAS No. : 2376198-66-0

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MAO-B-IN-6 相关抗体

Top Publications Citing Use of Products

查看 Monoamine Oxidase 亚型特异性产品:

查看所有亚型
MAO-A MAO-B

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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)[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 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

MAO-B-IN-6 相关抗体:
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].

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 / / 107.1
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
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.
纯度 & 产品资料
参考文献

MAO-B-IN-6 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MAO-B-IN-62376198-66-0Monoamine OxidaseMAOSafinamideParkinson's disease (PD)MPTP mouse Modeljaw movementscynomolgus monkeysdopamineselectiveorally activeSf9 cellsInhibitorinhibitorinhibit

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