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TRx0237 (LMTX) mesylate Microtubule Associated inhibitor

Name: TRx0237 (LMTX) mesylate
Brand: Selleck Chemicals
SKU: S7762
Rating: 5 (2 reviews)

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.

Chemical Structure

Molecular Weight: 477.62

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Quality Control

Batch: Purity: 99.36%

99.36

Related Targets	Akt Wnt/beta-catenin PKC HSP ROCK Integrin Bcr-Abl Actin FAK Kinesin
Other Microtubule Associated Inhibitors	Nocodazole MMAF Patupilone (Epothilone B) Lexibulin (CYT997) CW069 Combretastatin A4 Epothilone A ABT-751 (E7010) TAI-1 Cucurbitacin B

Chemical Information, Storage & Stability

Molecular Weight	477.62	Formula	C₁₆H₁₉N₃S.2CH₄O₃S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1236208-20-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
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
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	tau protein aggregation
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 form 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. 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.
In vivo	TRx 0237 dose-dependently rescues the learning impairment and restores behavioural flexibility in a spatial problem-solving water-maze task in L1 (minimum effective dose: 9 mg MT/kg for TRx0237) and corrects 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/26809554/ [2] http://www.alzforum.org/therapeutics/lmtm

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