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

Benztropine  (Synonyms: Benzatropine; Benzotropine)

Cat. No.: HY-B0520 Purity: 98.12%
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Benztropine (Benzatropine; Benzotropine) is an orally active and BBB-permeable centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine 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.

CAS No. : 86-13-5

Size Price Stock Quantity
Oil + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Benztropine:

Benztropine Related Antibodies

Top Publications Citing Use of Products

    Benztropine 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.

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    Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

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    mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target

    D2 Receptor

     

    In Vitro

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

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

    Benztropine Related Antibodies

    Cell Viability Assay[1]

    Cell Line: MDA-MB-231
    Concentration: 0, 0.1, 0.625, 1.25, 2.5, 5, 10 μM
    Incubation Time: 72 hours
    Result: Inhibited cells growth of MDA-MB-231 with an IC50 value about 5.0 μM.

    Cell Viability Assay[1]

    Cell Line: MDA-MB-231
    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 (5 μM, 4 weeks) inhibits tumor-initiating potential 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[1]
    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

    307.43

    Formula

    C21H25NO
    CAS No.
    Appearance

    Oil

    Color

    Colorless to light yellow

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage
    Pure form -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (325.28 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 3.2528 mL 16.2639 mL 32.5277 mL
    5 mM 0.6506 mL 3.2528 mL 6.5055 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    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: ≥ 2.5 mg/mL (8.13 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 (8.13 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.
    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.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    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).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    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. 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
    DMSO 1 mM 3.2528 mL 16.2639 mL 32.5277 mL 81.3193 mL
    5 mM 0.6506 mL 3.2528 mL 6.5055 mL 16.2639 mL
    10 mM 0.3253 mL 1.6264 mL 3.2528 mL 8.1319 mL
    15 mM 0.2169 mL 1.0843 mL 2.1685 mL 5.4213 mL
    20 mM 0.1626 mL 0.8132 mL 1.6264 mL 4.0660 mL
    25 mM 0.1301 mL 0.6506 mL 1.3011 mL 3.2528 mL
    30 mM 0.1084 mL 0.5421 mL 1.0843 mL 2.7106 mL
    40 mM 0.0813 mL 0.4066 mL 0.8132 mL 2.0330 mL
    50 mM 0.0651 mL 0.3253 mL 0.6506 mL 1.6264 mL
    60 mM 0.0542 mL 0.2711 mL 0.5421 mL 1.3553 mL
    80 mM 0.0407 mL 0.2033 mL 0.4066 mL 1.0165 mL
    100 mM 0.0325 mL 0.1626 mL 0.3253 mL 0.8132 mL
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    Benztropine 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:

    Benztropine86-13-5Benzatropine BenzotropineDopamine ReceptormAChRHistamine ReceptorMuscarinic acetylcholine receptorParkinson'sdiseaseanticholinergicdopaminetransporteranti-histamineInhibitorinhibitorinhibit

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