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编 号：F752527
分子式：C27H27FN4O2
分子量：458.53
分子式：C27H27FN4O2
分子量：458.53
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CAS No: 2417117-84-9
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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.
体内研究：
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。AChE/Nrf2 modulator 1 可显着降低小鼠模型大脑中促炎因子的水平。Animal Model:ICR mice
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.
体外研究：
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。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。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。
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.
体内研究：
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。AChE/Nrf2 modulator 1 可显着降低小鼠模型大脑中促炎因子的水平。Animal Model:ICR mice
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.
体外研究：
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。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。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。
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