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AChE/Nrf2 modulator 1

CAS No. : 2417117-84-9

MCE 站：AChE/Nrf2 modulator 1

产品活性：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。

研究领域：Neuronal Signaling  |  NF-κB

作用靶点：Cholinesterase (ChE)  |  Keap1-Nrf2

In Vitro: AChE/Nrf2 modulator 1 (Compound 15a) has significant Nrf2 inductivity ａnd excellent AChE inhibitory for eeAChE ａnd hAChE with IC₅₀ values of 0.07 μM ａnd 0.38 μM, respectively.
AChE/Nrf2 modulator 1 (5, 20 μM; 5-12 h) upregulates the protein ａnd transcription level of Nrf2 ａnd the downstream proteins HO1, NQO1, ａnd GCLM ａnd promotes Nrf2 translocation from cytoplasm into nuclei.
AChE/Nrf2 modulator 1 (1, 2.5, 5, 10, 20, 40 μM) exhibits important neuroprotective function in protecting the cells from being damaged by H202 ａnd Aβ1-42 aggregation ａnd exertes antioxidant stress ａnd anti-inflammatory activities in reducing the production of ROS ａnd pro-inflammatory cytokines.

In Vivo: AChE/Nrf2 modulator 1 (Compound 15a) (oral; 10 mg/kg; for 10 consecutive days) effectively shortens the latency time ａnd escape distance to the target, increased the arrival times, ａnd simplified the tracks in Morris water maze test induced by scopolamine ａnd Aβ1-42.
AChE/Nrf2 modulator 1 (10, 20 mg/kg; intragastric administration) significantly reduces the levels of proinflammatory factors in the mice model brains.

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