1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. Dopamine Receptor mAChR Histamine Receptor
  3. Benztropine mesylate

Benztropine mesylate  (Synonyms: Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate)

Cat. No.: HY-B0520A Purity: 99.92%
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Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects.

For research use only. We do not sell to patients.

Benztropine mesylate Chemical Structure

Benztropine mesylate Chemical Structure

CAS No. : 132-17-2

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Solid + Solvent
10 mM * 1 mL in DMSO
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5 g USD 50 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Benztropine mesylate:

Top Publications Citing Use of Products

    Benztropine mesylate purchased from MedChemExpress. Usage Cited in: Front Cell Neurosci. 2018 Sep 11;12:309.  [Abstract]

    p38MAPK activation by dopamine (DA) can be inhibited by selective DAT blockers (Benztropine and Vanoxerine; 2 μM each) and PMAT blocker (Decynium; 2 μM). Combination of DAT and PMAT blockers further inhibits the activation of p38MAPK.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[1][2].

    IC50 & Target[1]

    Human D2 Receptor

     

    In Vitro

    Benztropine mesylate (0.1-10 μM; 72 hours) treatment inhibits the cell growth of MDA-MB-231 cells with an IC50 of ~5 μM. In MDA-MB-231 cells and 4T1-luc2 cells, Benztropine mesylate reduces the size as well as the number of mammospheres significantly in a dose-dependent manne[1].
    ? Benztropine mesylate inhibits functions of cancer stem cells (CSCs) via the acetylcholine receptors, dopamine transporters/receptors, and/or histamine receptors[1].
    ? Benztropine mesylate induces the differentiation of oligodendrocytes through M1 and M3 muscarinic receptors and enhanced re-myelination[1].

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

    Cell Viability Assay[1]

    Cell Line: MDA-MB-231 cells
    Concentration: 0.1 μM, 0.625 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM
    Incubation Time: 72 hours
    Result: Inhibited the cell growth of MDA-MB-231 cells with an IC50 of ~5 μM.

    Cell Proliferation Assay[1]

    Cell Line: MDA-MB-231 cells
    Concentration: 0, 1, 2, 5 μM
    Incubation Time: 4-6 days
    Result: Suppressed mammosphere formation and self-renewal capacities of BCSCs in a dose-dependent manner in vitro.
    In Vivo

    Benztropine mesylate (1.5 mg/kg; daily; for 3 weeks; Balb/c mice) treatment significantly reduces both tumor size and tumor weight in a 4T1 mouse model[1].

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

    Animal Model: Balb/c mice bearing 4T1 breast tumors
    Dosage: 1.5 mg/kg
    Administration: Injection; 3 weeks
    Result: Reduced the tumor size and weight significantly without body weight changing.
    Clinical Trial
    Molecular Weight

    403.54

    Formula

    C22H29NO4S

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CN1[C@H]2CC(OC(C3=CC=CC=C3)C4=CC=CC=C4)C[C@@H]1CC2.CS(=O)(O)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    H2O : 100 mg/mL (247.81 mM; Need ultrasonic)

    DMSO : 100 mg/mL (247.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4781 mL 12.3903 mL 24.7807 mL
    5 mM 0.4956 mL 2.4781 mL 4.9561 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 (sealed storage, away from moisture). 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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    Volume (start)

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    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: ≥ 2.5 mg/mL (6.20 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.20 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 100 mg/mL (247.81 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: 99.92%

    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 (sealed storage, away from moisture). 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 2.4781 mL 12.3903 mL 24.7807 mL 61.9517 mL
    5 mM 0.4956 mL 2.4781 mL 4.9561 mL 12.3903 mL
    10 mM 0.2478 mL 1.2390 mL 2.4781 mL 6.1952 mL
    15 mM 0.1652 mL 0.8260 mL 1.6520 mL 4.1301 mL
    20 mM 0.1239 mL 0.6195 mL 1.2390 mL 3.0976 mL
    25 mM 0.0991 mL 0.4956 mL 0.9912 mL 2.4781 mL
    30 mM 0.0826 mL 0.4130 mL 0.8260 mL 2.0651 mL
    40 mM 0.0620 mL 0.3098 mL 0.6195 mL 1.5488 mL
    50 mM 0.0496 mL 0.2478 mL 0.4956 mL 1.2390 mL
    60 mM 0.0413 mL 0.2065 mL 0.4130 mL 1.0325 mL
    80 mM 0.0310 mL 0.1549 mL 0.3098 mL 0.7744 mL
    100 mM 0.0248 mL 0.1239 mL 0.2478 mL 0.6195 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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    • 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.

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