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CAS No. : 2254492-08-3
MCE 国际站:NXPZ-2
产品活性:NXPZ-2 是一种具有口服活性的 Keap1-Nrf2 protein–protein interaction(PPI) 抑制剂,Ki 值为95 nM,EC50 值为 120 和 170 nM。NXPZ-2 可剂量依赖性地缓解 Aβ 诱导的认知紊乱,并通过增加神经元数量和功能提高阿尔茨海默病 (AD) 小鼠脑组织的病理改变情况。NXPZ-2 可通过上调 Nrf2 含量并促进其从细胞质向细胞核的易位来抑制氧化应激,有助于 Keap1-Nrf2 PPI 抑制剂和 AD 相关的疾病研究。
研究领域:NF-κB
作用靶点:Keap1-Nrf2
In Vitro: NXPZ-2 (0-200 μM, 7 days) has no obvious toxicity on primary cortical neuron.
In Vivo: NXPZ-2 (Male ICR mice, 52.5/105/210 mg/kg, p.o., once daily for 7 days) improves AD mice learning and memorizing function including increased spontaneous alternation, increases number of active avoidance times, shortened escape latency, increased the time spent in the target quadrant and number of platform crossing.NXPZ-2 (Male ICR mice, 52.5/105/210 mg/kg, p.o., once daily for 7 days) rescues the brain structure damage and lowers dead neuron numbers of AD mice with no obvious toxicity on mouse organs.NXPZ-2 (Male ICR mice, 52.5/105/210 mg/kg, p.o., once daily for 7 days) alleviates oxidative stress by increasing Nrf2 expression levels, and promotes Nrf2’s cytoplasm to nuclear translocation, and improves cognitive dysfunction by elevating Nrf2 in both the central nervous system and peripheral blood.
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