Nrf2-ARE/hMAO-B/QR2 modulator 1是一种新的基于白藜芦醇的多靶点定向配体(MTDL)，显示出良好的平衡MTDL特征:细胞激活Nrf2-ARE通路(CD = 9.83 μM)，选择性抑制hMAO-B和QR2 (IC50s = 8.05和0.57 μM)，并具有最佳的促进海马神经发生的能力。Nrf2-ARE/hMAO-B/QR2调节剂1在急性和慢性阿尔茨海默症模型中使用海马组织发挥神经保护和抗氧化作用。

Nrf2-ARE/hMAO-B/QR2 modulator 1 is a new resveratrol-based multitarget-directed ligands (MTDLs) that showed a well-balanced MTDL profile: cellular activation of the NRF2-ARE pathway (CD = 9.83 μM), selective inhibition of both hMAO-B and QR2 (IC50s = 8.05 and 0.57 μM), and the best ability to promote hippocampal neurogenesis. Nrf2-ARE/hMAO-B/QR2 modulator 1 exerts neuroprotective and antioxidant actions in both acute and chronic Alzheimer models using hippocampal tissues.

Nrf2-ARE/hMAO-B/QR2 modulator 1 (compound 4e) (100 μM; 24 hours) reduces the viability of SH-SY5Y cells by around 30% in MTT assay[1]. Nrf2-ARE/hMAO-B/QR2 modulator 1 (1 μM; 24 hours for pre-treatment, then coincubated for another 24 hours with 10 nM okadaic acid (OA)) significantly increases the cell viability of OA-treated rat primary cortical neurons to 70-80% while OA (10 nM) reduced the cell viability by 50%[1]. Nrf2-ARE/hMAO-B/QR2 modulator 1 (10 μM) shows the highest expression of young cells (TuJ-1) and mature neurons (MAP-2), as well as the greatest distance of cell migration which indicate that this compound has a great neurogenic potential due to its ability to promote different aspects involved in neurogenesis[1]. Nrf2-ARE/hMAO-B/QR2 modulator 1 (1 μM; 72 hours) confers neuroprotection and reduces cell death, significantly reduces ROS production in mice hippocampal slices exposed to OA [1].

C14H12N2O3

256.26

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