2. Neuronal Signaling NF-κB
  3. Cholinesterase (ChE) Keap1-Nrf2
  4. AChE/Nrf2 modulator 1

AChE/Nrf2 modulator 1 是乙酰胆碱酯酶 (AChE) /核因子红系 2 相关因子 2 (Nrf2) 调节剂，具有口服活性。AChE/Nrf2 modulator 1 具有 Nrf2 诱导活性和 AChE 抑制活性，对 eeAChE 和 hAChE 的 IC50 值分别为 0.07 μM 和 0.38 μM。AChE/Nrf2 modulator 1 可用于阿尔茨海默病的研究。

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AChE/Nrf2 modulator 1 Chemical Structure

AChE/Nrf2 modulator 1 Chemical Structure

CAS No. : 2417117-84-9

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AChE/Nrf2 modulator 1 相关抗体

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AChE BChE

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AChE/Nrf2 modulator 1 is an orally active acetylcholinesterase (AChE)/nuclear factor erythroid 2-related factor 2 (Nrf2) modulator. AChE/Nrf2 modulator 1 has Nrf2 inductive activity and AChE inhibitory activity for eeAChE and hAChE with IC50 values of 0.07 μM and 0.38 μM, respectively. AChE/Nrf2 modulator 1 can be used for the research of Alzheimer's disease[1].

IC50 & Target

IC50: 0.07 μM (eAChE); 0.38 μM (hAChE)[1]
体外研究
(In Vitro)

AChE/Nrf2 modulator 1 (Compound 15a) 具有显着的 Nrf2 诱导性， 对 eeAChE 和 hAChE 具有出色的 AChE 抑制作用，IC50 值分别为 0.07 μM 和 0.38 μM[1]。
AChE/Nrf2 modulator 1 (5, 20 μM; 5-12 h) 上调 Nrf2 及其下游蛋白 HO1、NQO1 和 GCLM 的蛋白和转录水平，促进 Nrf2 从细胞质转运到细胞核[1]。
AChE/Nrf2 modulator 1 (1, 2.5, 5, 10, 20, 40 μM) 在保护细胞免受 H2O2 和 Aβ1-42 聚集的损害方面表现出重要的神经保护功能，发挥抗氧化应激和抗炎活性，减少 ROS 和促炎细胞因子的产生[1]。

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

AChE/Nrf2 modulator 1 相关抗体:

Western Blot Analysis[1]

Cell Line: PC12 cells
Concentration: 20 μM; 5, 20 μM
Incubation Time: 5-10 h; 6 h
Result: Significantly activated the expression of Nrf2 downstream proteins.
Increase the level of Nrf2 and its downstream protein HO-1, NQO1, and GCLM in a dose-dependent manner at 6 h.
Increased the translocation of Nrf2 into the nucleus.

RT-PCR[1]

Cell Line: PC12 cells
Concentration: 20 μM
Incubation Time: 0, 1, 2, 5, 10, 24 h
Result: Increased the Nrf2, HO-1, NQO1, and GCLM gene expression in dose dependent manner.

Immunofluorescence[1]

Cell Line: PC12 cells
Concentration: 5, 20 μM
Incubation Time: 12 h
Result: Induced the Nrf2 translocation into the nucleus in dose dependent manner.
体内研究
(In Vivo)

AChE/Nrf2 modulator 1 (Compound 15a) (口服；10 mg/kg；连续10天) 有效缩短了潜伏期和逃逸到目标的距离，增加了到达时间，并简化了由 scopolamine 和 Aβ1-42 诱导的 Morris 水迷宫试验中的轨迹[1]。
AChE/Nrf2 modulator 1 可显着降低小鼠模型大脑中促炎因子的水平[1]。

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

Animal Model: ICR mice[1]
Dosage: 10, 20 mg/kg
Administration: Intragastric administration; oral; for 10 consecutive days
Result: Significantly reduced the latency time to target and simplified the traveled distance and exhibited a good effect on ameliorating ethological changes and spatial memory impairment by rescuing cholinergic function
. Showed an obvious reduction of pro-inflammation factors level and significantly increased the content of TGF-β1.
分子量

458.53

Formula

C27H27FN4O2
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/Nrf2 modulator 1 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

AChE/Nrf2 modulator 12417117-84-9Cholinesterase (ChE)Keap1-Nrf2Designing of multiple-target directed ligands (MTDLs)Alzheimer's disease (AD)acetylcholinesterase (AChE)nuclear factor erythroid 2-related factor 2 (Nrf2)eeAChEhAChEInhibitorinhibitorinhibit

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