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。
| 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 andAChEinhibitory activity for eeAChE and hAChE withIC50values 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]。
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. |
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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]。
| 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
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Showed an obvious reduction of pro-inflammation factors level and significantly increased the content of TGF-β1. |
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| 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. |
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