2. Neuronal Signaling
  3. Amyloid-β
  4. Leucomethylene blue mesylate

Leucomethylene blue mesylate  (Synonyms: TRx0237 mesylate; Methylene blue leuco base mesylate)

Cat. No.: HY-19948 Purity: 98.75%
COA Handling Instructions

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Leucomethylene blue (TRx0237) mesylate, an orally active second-generation tau protein aggregation inhibitor (Ki of 0.12 μM), could be used for the study of Alzheimer's Disease. Leucomethylene blue mesylate is a common reduced form of Methylene Blue, Methylene Blue is a member of the thiazine class of dyes.

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Leucomethylene blue mesylate Chemical Structure

Leucomethylene blue mesylate Chemical Structure

CAS No. : 1236208-20-0

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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Leucomethylene blue mesylate:

Leucomethylene blue mesylate Related Antibodies

Top Publications Citing Use of Products

    Leucomethylene blue mesylate purchased from MedChemExpress. Usage Cited in: Bioorg Med Chem. 2018 Sep 1;26(16):4693-4705.  [Abstract]

    Imaging of HEK-293T cells incubated with or without LMTM (0.5 μM) and 30 (1 μM).

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Leucomethylene blue (TRx0237) mesylate, an orally active second-generation tau protein aggregation inhibitor (Ki of 0.12 μM), could be used for the study of Alzheimer's Disease. Leucomethylene blue mesylate is a common reduced form of Methylene Blue, Methylene Blue is a member of the thiazine class of dyes[1][2][3].

    IC50 & Target

    Ki: 0.12 μM (tau)[3].
    In Vitro

    Leucomethylene blue (100 nM, 48 h) mesylate not only decreases the tau and p-tau expression levels, but also reverses the promoting effects of Aβ25-35 on orexin A and adenosine A1R expression levels[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Leucomethylene blue mesylate Related Antibodies

    Western Blot Analysis[2]

    Cell Line: Human SH-SY5Y cell line.
    Concentration: 100 nM.
    Incubation Time: 48 h.
    Result: Aβ25-35 and TRx 0237 co-treatment significantly reversed the promoting effects of Aβ25-35 on tau, p-tau, orexin A and adenosine A1R expression.
    Clinical Trial
    Molecular Weight

    477.62

    Formula

    C18H27N3O6S3
    CAS No.
    Appearance

    Solid

    Color

    Light green to green

    SMILES

    CN(C)C1=CC(SC2=CC(N(C)C)=CC=C2N3)=C3C=C1.CS(=O)(O)=O.CS(=O)(O)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, protect from light, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    DMSO : 110 mg/mL (230.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 83.33 mg/mL (174.47 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0937 mL 10.4686 mL 20.9371 mL
    5 mM 0.4187 mL 2.0937 mL 4.1874 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 7.5 mg/mL (15.70 mM); Clear solution

      This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.75 mg/mL (5.76 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 50 mg/mL (104.69 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation

    Purity: 98.75%

    COA (253 KB) HNMR (130 KB) RP-HPLC (233 KB) MS (70 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 2.0937 mL 10.4686 mL 20.9371 mL 52.3429 mL
    5 mM 0.4187 mL 2.0937 mL 4.1874 mL 10.4686 mL
    10 mM 0.2094 mL 1.0469 mL 2.0937 mL 5.2343 mL
    15 mM 0.1396 mL 0.6979 mL 1.3958 mL 3.4895 mL
    20 mM 0.1047 mL 0.5234 mL 1.0469 mL 2.6171 mL
    25 mM 0.0837 mL 0.4187 mL 0.8375 mL 2.0937 mL
    30 mM 0.0698 mL 0.3490 mL 0.6979 mL 1.7448 mL
    40 mM 0.0523 mL 0.2617 mL 0.5234 mL 1.3086 mL
    50 mM 0.0419 mL 0.2094 mL 0.4187 mL 1.0469 mL
    60 mM 0.0349 mL 0.1745 mL 0.3490 mL 0.8724 mL
    80 mM 0.0262 mL 0.1309 mL 0.2617 mL 0.6543 mL
    100 mM 0.0209 mL 0.1047 mL 0.2094 mL 0.5234 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Leucomethylene blue mesylate Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Leucomethylene blue1236208-20-0TRx0237Methylene blue leuco baseTRx 0237TRx-0237Amyloid-ββ-amyloid peptideAβAbetaTauaggregationAlzheimer'sDiseaseAβ25-35Inhibitorinhibitorinhibit

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