2. Neuronal Signaling
  3. Cholinesterase (ChE) Monoamine Oxidase Amyloid-β Tau Protein
  4. AChE/MAO-B-IN-9

AChE/MAO-B-IN-9 (Compound E12) 是一种具有口服活性的、选择性的、可逆的、非竞争性的 AChE 和 MAO-B 抑制剂，其对电鳗 AChE 的 IC50 为 0.156 μM。AChE/MAO-B-IN-9 可抑制 Aβ40/42 原纤维形成、促进 Aβ 原纤维解聚、抑制 Tau 蛋白原纤维形成。AChE/MAO-B-IN-9 发挥抗氧化和神经保护作用，并可改善 Scopolamine (HY-N0296) 诱导的小鼠记忆障碍。AChE/MAO-B-IN-9 可用于阿尔茨海默病的研究。

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AChE/MAO-B-IN-9

AChE/MAO-B-IN-9 Chemical Structure

CAS No. : 2341935-88-2

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AChE/MAO-B-IN-9 相关抗体

Top Publications Citing Use of Products

查看 Cholinesterase (ChE) 亚型特异性产品:

查看所有亚型
AChE BChE

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

AChE/MAO-B-IN-9 (Compound E12) is an orally active, selective, reversible, non-competitive AChE and MAO-B inhibitor, with an IC50 of 0.156 μM against electric eel AChE. AChE/MAO-B-IN-9 inhibits Aβ40/42 fibril formation, promotes Aβ fibril depolymerization, and inhibits Tau protein fibril formation. AChE/MAO-B-IN-9 exerts antioxidant and neuroprotective effects, and improves scopolamine (HY-N0296)-induced memory impairment in mice. AChE/MAO-B-IN-9 can be used for the research of Alzheimer's disease[1].

IC50 & Target[1]

MAO-B

 

EeAChE

0.156 μM (IC50)

体外研究
(In Vitro)

AChE/MAO-B-IN-9 (12 min) 可强效抑制电鳗 AChE，其 IC50 为 0.156 ± 0.11 μM，且对 AChE 的选择性比对 BuChE 高 36.79 倍[1]。
AChE/MAO-B-IN-9 (1 μM; 60 min) 可使小鼠肝脏线粒体 MAO-B 的活性被抑制 54.9 ± 2.7%[1]。
AChE/MAO-B-IN-9 (0.625-10 μM; 最多 80 h) 可浓度依赖性地抑制 Aβ40 纤维形成，其 IC50 为 10.00 μM[1]。
AChE/MAO-B-IN-9 (0.625-10 μM; 最多 80 h) 可以浓度依赖的方式强效抑制 Aβ42 纤维形成，其 IC50 为 1.01 μM[1]。
AChE/MAO-B-IN-9 (2.5-10 μM; 最多 50 h) 可抑制 Tau 蛋白纤维形成，其 IC50 为 4.50 μM，在 10 μM 浓度下可使平台期荧光强度降低 49%[1]。
AChE/MAO-B-IN-9 (1.25-20 μM; 24 h) 可呈浓度依赖性抑制 SH-SY5Y 细胞的 Aβ 分泌，在 20 μM 作用 24 h 后对总 Aβ 的抑制率约达 80%[1]。

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

AChE/MAO-B-IN-9 相关抗体:

Cell Viability Assay[1]

Cell Line: SH-SY5Y cells
Concentration: 10-20 μM
Incubation Time: 24 h
Result: Maintained cell viability within normal ranges (94-97%) when used alone.
Significantly counteracted Aβ40 and Aβ42 oligomer-induced toxicity, restoring cell survival toward control levels.
体内研究
(In Vivo)

AChE/MAO-B-IN-9 (1-5 mg/kg；口服；每日一次；7天) 可呈剂量依赖性改善 Scopolamine (HY-N0296) 诱导的雄性 ICR 小鼠空间记忆障碍[1]。

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

Animal Model: ICR mice (male, 8 weeks old, SPF-grade)[1]
Dosage: 1 mg/kg; 5 mg/kg
Administration: p.o.; daily; 7 days
Result: Maintained stable body weights with minimal fluctuations relative to baseline.
Averaged 3.1 platform crossings at 1 mg/kg dose in Morris water maze test.
Averaged 3.9 platform crossings at 5 mg/kg dose in Morris water maze test.
Showed highly directed, efficient pathing toward the target quadrant on Day 5 at 5 mg/kg dose.
Caused no pathological alterations in heart, liver, spleen, lung, and kidney tissues.
分子量

381.40

Formula

C21H20FN3O3
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

AChE/MAO-B-IN-9 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

AChE/MAO-B-IN-92341935-88-2Cholinesterase (ChE)Monoamine OxidaseAmyloid-βTau ProteinMAOβ-amyloid peptideAβAbetaMAO-AbutyrylcholinesteraseTaumicemonoamine oxidase-BElectric EelacetylcholinesteraseSH-SY5Y cellsAlzheimer's diseaseAβ40/42Inhibitorinhibitorinhibit

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