TRx0237 mesylate 是一种 Methylene blue (亚甲基蓝)的还原形式, 亚甲基蓝是一种化学指示剂和生物染色剂。它是一种具有口服活性的二代tau蛋白聚集的抑制剂 (Ki=为0.12 μM)，可用于阿尔兹海默症的研究。

TRx 0237 (LMTX) mesylate is a second-generation tau protein aggregation inhibitor for the treatment of Alzheimer's disease (AD) and frontotemporal dementia.

TRx 0237 (LMTX?) is a second-generation tau protein aggregation inhibitor for the treatment of Alzheimer's disease (AD) and frontotemporal dementia. It is a purified forms of Methylene Blue, an old drug that predates the FDA and is being widely used in Africa for the treatment for malaria as well as for methemoglobinemia and other conditions[2]. An in vitro study showed the ability of TRx 0237 in disrupting PHFs(paired helical filaments) isolated from Alzheimer's Disease brain tissues at the concentration at 0.16 μM[1].

TRx 0237 dose-dependently rescues the learning impairment and restores behavioral flexibility in a spatial problem-solving water-maze task in L1 (minimum effective dose: 9 mg MT/kg for TRx0237) and correctes motor learning in L66 (effective doses: 4 mg MT/kg). It reduces the number of tau-reactive neurons, particularly in the hippocampus and entorhinal cortex in L1 and in a more widespread manner in L66[1].

1236208-20-0

C18H27N3O6S3

477.61

TRx0237 (LMTX) mesylate;Leucomethylene Blue Dimesylate;Methylene blue leuco base mesylate salt;TRx0237 mesylate;N3,N3,N7,N7-四甲基-10H-吩噻嗪-3,7-二胺二甲磺酸盐

Ethanol:<1 mgml
DMSO:88 mg/mL (184.2 mM)
H2O:87 mg/mL (182.2 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years