| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
TRX-0237 mesylate (LMT-X; TRX0237; Leuco-MTx; LMTX; Hydromethylthionine mesylate), the mesylate salt of TRX 0237 which is currently in phase III clinical trials by TauRx, is a 2nd-generation tau protein aggregation and TDP-43 aggregation inhibitor with the potential for the treatment of Alzheimer's disease (AD) and frontotemporal dementia. It is a replacement formulation for Rember®, the first company's first proprietary formulation of methylthioninium chloride (MTC). Both TRx 0237 and Rember are 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. TRx 0237 and Rember share the same mode of action, but TRx 0237 has been designed as a stabilized, reduced form of MTC to improve the drug's absorption, bioavailability, and tolerability.
| ln Vitro |
In addition to lowering tau and p-tau expression levels, colorless methylene blue (100 nM, 48 h) methanesulfonate also undid the encouraging effects of Aβ25-35 on beta-A and adenosine A1R expression levels [2]. [
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|---|---|
| Cell Assay |
Western Blot Analysis[2]
Cell Types: human SH-SY5Y cell line. Tested Concentrations: 100 nM. Incubation Duration: 48 hrs (hours). Experimental Results: Co-treatment of Aβ25-35 and TRx 0237 Dramatically reversed the promoting effect of Aβ25-35 on the expression of tau, p-tau, orexin A and adenosine A1R. |
| References |
[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. |
| Molecular Formula |
C17H21N3O3S2
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|---|---|
| Molecular Weight |
379.493
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| CAS # |
1236208-20-0
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| Related CAS # |
613-11-6;1236208-20-0 (mesylate);61-73-4 (chloride);951131-15-0 (HBr);
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
CN(C1=CC(SC2=CC(N(C)C)=CC=C2N3)=C3C=C1)C.OS(=O)(C)=O.OS(=O)(C)=O
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| InChi Key |
SPCMQFLNOVTUBM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H19N3S.2CH4O3S/c1-18(2)11-5-7-13-15(9-11)20-16-10-12(19(3)4)6-8-14(16)17-132*1-5(2,3)4/h5-10,17H,1-4H32*1H3,(H,2,3,4)
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| Chemical Name |
3,7-bis(dimethylamino)phenothiazin-5-ium methanesulfonate
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| Synonyms |
TRX-0237 LMTX. L-MTx LMT-X TRX 0237 TRX0237Leuco-MTx Methylene blue mesylate. Leuco-methylonium bis(hydromethanesulfonate)
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~110 mg/mL (~230.31 mM)
H2O : ~83.33 mg/mL (~174.47 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 7.5 mg/mL (15.70 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 75.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.75 mg/mL (5.76 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 50 mg/mL (104.69 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6351 mL | 13.1756 mL | 26.3512 mL | |
| 5 mM | 0.5270 mL | 2.6351 mL | 5.2702 mL | |
| 10 mM | 0.2635 mL | 1.3176 mL | 2.6351 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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