2. Neuronal Signaling
  3. Monoamine Oxidase
  4. MAO-B-IN-20

MAO-B-IN-20 (Compound C14) 是一种有效的 MAO-B 抑制剂，IC50 为 0.037 μM。MAO-B-IN-20 表现出良好的代谢稳定性和脑血屏障渗透性。MAO-B-IN-20 可用于帕金森病的研究。

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MAO-B-IN-20 Chemical Structure

MAO-B-IN-20 Chemical Structure

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MAO-B-IN-20 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-20 (Compound C14) is a potent MAO-B inhibitor with an IC50 of 0.037 μM. MAO-B-IN-20 displays good metabolic stability and brain-blood barrier permeability. MAO-B-IN-20 can be used for the research of Parkinson's disease[1].

IC50 & Target[1]

MAO-B

0.037 μM (IC50)

MAO-A

>10 μM (IC50)

体外研究
(In Vitro)

MAO-B-IN-20 (Compound C14) 与 MAO-B 的活性位点结合，与 Safinamide (HY-70057) 具有相似的结合模式[1]。

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

MAO-B-IN-20 相关抗体:
体内研究
(In Vivo)

MAO-B-IN-20 (Compound C14; 5 mg/kg; i.v.) 在 15 分钟内迅速被吸收并穿越血脑屏障，60 分钟内在血浆和脑中达到 Cmax。MAO-B-IN-20 在 60 分钟内表现出适当的脑浆比为 16.20，并且在脑中具有高浓度 (8753 ng/g)[1]。
MAO-B-IN-20 (0.08-1.28 mg/kg; i.p.; once) 以剂量依赖的方式显著抑制小鼠脑中的 MAO-B 活性[1]。
MAO-B-IN-20 (0.3-3 mg/kg; i.p.; once) 在 MPTP（HY-15608） 诱导的小鼠模型中显示出对多巴胺缺陷的潜在效果，并且显著增加了纹状体中的多巴胺浓度[1]。
Pharmacokinetic profile of MAO-B-IN-20 (Compound C14) in SD ratsa[1]

Compound Route Dose (mg/kg) Cmax (ng/mL) AUCt (ng•h/mL) T1/2 (h) Vss (L/kg) CL (mL/min/kg) F (%)
MAO-B-IN-20 (Compound C14) iv 1 273 305 0.74 3.33 54.2 /
ig 5 436 2280 4.22 / / 149.5

aFasted male SD rats. Dosing volumes: 5 mL/kg for ig and 1 mL/kg for iv. Cmax: Maximum Concentration, AUCt: Area under the plasma concentration-time curve from time 0 to last time of quantifiable concentration; T1/2: Elimination half time, Vss: Steady-state distribution volume, CL: plasma clearance, F: bioavailability.
Pharmacokinetic profile of MAO-B-IN-20 (Compound C14) in ICR micea[1]
Compound Route Dose (mg/kg) Cmax (ng/mL) AUCt (ng•h/mL) T1/2 (h) Vss (L/kg) CL (mL/min/kg) F (%)
MAO-B-IN-20 (Compound C14) iv 2 900 2680 3.37 2.72 11 /
ig 5 913 7950 3.80 / / 104.8

aFasted male ICR mice. Dosing volumes: 5 mL/kg for ig and 2 mL/kg for iv. Cmax: Maximum Concentration, AUCt: Area under the plasma concentration-time curve from time 0 to last time of quantifiable concentration; T1/2: Elimination half time, Vss: Steady-state distribution volume, CL: plasma clearance, F: bioavailability.

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

Animal Model: MPTP-induced acute mouse model of PD[1]
Dosage: 0.3, 1.0, 3.0 mg/kg
Administration: Intraperitoneal injection, 30 min before MPTP (20 mg/kg, ip) injection
Result: Dopamine concentration in the striatum of mice significantly increased compared with the MPTP-alone-injected group.
Animal Model: SD rats and ICR mice[1]
Dosage: 1, 2 and 5 mg/kg
Administration: IV and IG (Pharmacokinetic Analysis)
Result: Showed good pharmacokinetic profiles.
分子量

356.37

Formula

C20H18F2N2O2
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-20 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)

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The dilution calculator equation

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

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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-20Monoamine OxidaseMAOParkinson's diseaseSafinamideMPTPdopamineInhibitorinhibitorinhibit

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