AChE/Nrf2 modulator 1_product_DataBase

Bioactivity	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].
Target	IC50: 0.07 μM (eAChE); 0.38 μM (hAChE)
Invitro	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:
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:
Name	AChE/Nrf2 modulator 1
CAS	2417117-84-9
Formula	C27H27FN4O2
Molar Mass	458.53
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Yuanyuan Wang, et al. Design, synthesis and evaluation of fused hybrids with acetylcholinesterase inhibiting and Nrf2 activating functions for Alzheimer's disease. Eur J Med Chem. 2022 Dec 15;244:114806.

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AChE/Nrf2 modulator 1

CAS: 2417117-84-9 F: C27H27FN4O2 W: 458.53