Biological Activity
TRx 0237 mesylate (LMTX, Hydromethylthionine) is a second-generation tau protein aggregation inhibitor. For the treatment of Alzheimer's disease and frontotemporal dementia.
in vitro
TRx 0237 (LMTX?) is a second-generation tau aggregation inhibitor for the treatment of Alzheimer's disease and frontotemporal dementia. It is a purified form of methylene blue, an ancient drug widely used in Africa to treat malaria and methemoglobinemia. In vitro experiments demonstrated that 0.16 μM TRx 0237 interfered with double helical filaments (PHF) isolated from Alzheimer's disease patient brain tissue.
in vivo
TRX-0237 mesylate dose-dependently rescues learning impairment in L1 (a mouse strain overexpressing truncated tau protein) and restores its behavioral resilience in the water maze test (minimum dose administered: 9 mg MT/kg). In L66 (a mouse strain overexpressing full-length tau-P301S/G335D), it modulates its motor learning (effective dose: 4 mg MT/kg). It reduced the number of tau-active neurons, especially in the hippocampus and entorhinal cortex of L1, and more generally in the L66 strain.
target
| Target | Value |
| tau protein aggregation |
