Tideglusib(又名NP031112, NP-12)是小杂环噻二唑烷酮(TDZD)的衍生物,是不可逆的、非ATP竞争性的GSK-3β抑制剂,能够抑制GSK-3β WT和GSK-3β C199A,IC50值分别为5 nM和60 nM。目前正处于阿尔茨海默氏症和进行性核上性麻痹(PSP)临床试验阶段研究。Tideglusib可减少tau蛋白的磷酸化和淀粉样斑块的积聚,减少海马和内嗅皮层神经元的丢失并改善空间记忆缺陷,在多种动物模型中也显示出神经保护和抗炎活性。
参考文献
[1].Domínguez JM, et al. Evidence for irreversible inhibition of glycogen synthase kinase-3 by Tideglusib. J Biol Chem. 2012;287(2):893-904.
[2].Serenóa L, et al. A novel GSK-3β inhibitor reduces Alzheimer's pathology and rescues neuronal loss in vivo. Neurobiol Dis. 2009;35(3):359-67.
[3].Luna-Medina R, et al. NP031112, a thiadiazolidinone compound, prevents inflammation and neurodegeneration under excitotoxic conditions: potential therapeutic role in brain disorders. J Neurosci. 2007;27(21):5766-76.
冰袋运输。粉末直接保存于-25~-15℃,有效期2年。建议干燥避光保存,避免反复冻融。