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TRx0237 (LMTX) mesylate Microtubule Associated inhibitor

Cat.No.S7762

TRx 0237 mesylate (LMTX, Hydromethylthionine) is a second-generation tau protein aggregation inhibitor for the treatment of Alzheimer's disease (AD) and frontotemporal dementia.
TRx0237 (LMTX) mesylate Microtubule Associated inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 477.62

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 477.62 Formula

C16H19N3S.2CH4O3S

Storage (From the date of receipt)
CAS No. 1236208-20-0 Download SDF Storage of Stock Solutions

Synonyms Hydromethylthionine mesylate Smiles CN(C)C1=CC2=C(C=C1)NC3=C(S2)C=C(C=C3)N(C)C.CS(=O)(=O)O.CS(=O)(=O)O

Solubility

In vitro
Batch:

DMSO : 96 mg/mL (200.99 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 96 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
tau protein aggregation [1]
In vitro
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].
In vivo
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].
References

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