CAS:1236208-20-0
品牌:MedChemExpress (MCE)
存储条件:4°C, stored under nitrogen, away from moisture
生物活性:Leucomethylene blue (TRx0237) mesylate 是一种具有口服活性的第二代 tau 蛋白聚集抑制剂(Ki 为 0.12 μM),可用于阿尔茨海默病的研究。甲磺酸无色亚甲蓝是亚甲蓝的常见还原形式,亚甲蓝是噻嗪类染料的成员[1][2] 。 IC50 和目标:Ki:0.12 μM (tau)[3]。
体外:Leucomethylene blue (100 nM, 48 h) mesylate 不仅降低了 tau 和 p-tau 的表达水平,而且逆转了 Aβ25-35 对食欲素 A 和腺苷 A1R 表达水平的促进作用[2] .
参考详情:www.medchemexpress.com/Leucomethylene-blue-Mesylate.html
参考文献:
[1]. Gaudette NF, et al. Determination of methylene blue and leucomethylene blue in male and female Fischer 344 rat urine andB6C3F1 mouse urine. J Anal Toxicol. 2005 Jan-Feb;29(1):28-33.
[2]. Zhenhua Liu, et al. Amyloid β and tau are involved in sleep disorder in Alzheimer's disease by orexin A and adenosine A(1) receptor. Int J Mol Med. 2019 Jan;43(1):435-442.
[3]. Francesco Panza, et al. Tau aggregation inhibitors: the future of Alzheimer's pharmacotherapy? Expert Opin Pharmacother. 2016;17(4):457-61.