1. Neuronal Signaling
  2. Cholinesterase (ChE)
  3. AChE-IN-24

AChE-IN-24 是一种有效的 AChE 抑制剂,可以穿透血脑屏障。AChE-IN-24 对 hAChE 具有较强的抑制活性,其 IC50 值为 0.053 μM。AChE-IN-24 可用于阿尔茨海默病 (AD) 的研究。

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AChE-IN-24 Chemical Structure

AChE-IN-24 Chemical Structure

CAS No. : 3033542-32-1

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查看 Cholinesterase (ChE) 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AChE-IN-24 is a potent AChE inhibitor and can penetrate the BBB. AChE-IN-24 has the mighty inhibitory activity to hAChE with an IC50 value of 0.053 μM. AChE-IN-24 can be used for the research of Alzheimer s disease (AD)[1].

IC50 & Target

AChE

 

体外研究
(In Vitro)

AChE-IN-24 (compound 4c2) has good hAChE inhibitory activity with IC50values of 0.053 μM but owns little inhibition to hBuChE[1].
AChE-IN-2 has inhibitory activity for electric eel acetylcholinesterase (eeAChE) and equine serum butyrylcholinesterase (eqBuChE) with IC50values of 0.088 μM and 7.5μM, respectively[1].
AChE-IN-24 (0-0.2 μM) can cross the BBB comfortably by means of passive diffusion[1].
AChE-IN-2 (0-40 μM) triggers the translocation of Nrf2 to the nucleus, thereby expediting the binding of Nrf2 to the ARE for the transcription process[1].
AChE-IN-2 (7 μM) significantly induces the expression of antioxidant-related enzymes by activating Nrf2 in BV-2 cells[1].
AChE-IN-2 (1, 3, 7 μM) protects cells from H2O2-induced damage and inhibits ROS accumulation[1].
AChE-IN-2 (1, 3, 7 μM) attenuates inflammatory responses[1].

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

Cell Viability Assay[1]

Cell Line: BV-2 microglial cells
Concentration: 0, 2.5, 5, 10, 20 and 40 μM
Incubation Time: 24 h
Result: Not observed significant cytotoxicity.

Western Blot Analysis[1]

Cell Line: BV-2 microglial cells
Concentration: 7 μM
Incubation Time: 0-15 h
Result: Up-regulated the amount of total Nrf2 in a time-dependent manner, decreased gradually the cytosolic Nrf2 level with its continuous accumulation in the nucleus and increased the total cellular Nrf2 accumulation in concentration-dependently.
Increased the protein expression levels of HO-1, NQO1, and GPX4 in a concentration-dependent manner with the biggest upregulation observed at 10 μM and significantly increased the protein levels of HO-1, NQO1, and GPX4 reaching the maximum at 9h, 6 h, and 3 h, respectively[1].
体内研究
(In Vivo)

AChE-IN-24 (compound 4c2) (oral; 0, 625, 1250, and 2500 mg/kg) is well tolerated and no toxicity in KM mice[1].
AChE-IN-24 (7.5 mg/kg, 15 mg/kg and 30mg/kg; once) ameliorates cognitive deficit induced by Scopolamine, suggesting a practicable therapeutic effect on AD[1].

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

Animal Model: KM mice[1]
Dosage: 0, 625, 1250, and 2500 mg/kg
Administration: oral; 0, 625, 1250, and 2500 mg/kg
Result: Not discovered abnormal behavior and acute toxicity were monitored for the first 4 h after administration, no acute neurological toxicities inclusive of tremor, convulsion, and death and no obvious signs of poisoning in the heart, liver, lungs, kidneys, and brain.
Animal Model: The cognitive deficit mice model[1]
Dosage: 7.5 mg/kg, 15 mg/kg and 30mg/kg
Administration: 7.5 mg/kg, 15 mg/kg and 30mg/kg; once
Result: Reversed the step-down latency and number of errors in a concentration-dependent manner.
分子量

450.61

Formula

C22H30N2O4S2

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-IN-24 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

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HY-151152
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