2. Neuronal Signaling
  3. Dopamine Transporter
  4. Vanoxerine dihydrochloride

Vanoxerine dihydrochloride  (Synonyms: GBR-12909 dihydrochloride; I893 dihydrochloride)

Cat. No.: HY-13217 Pureté: 99.60%
COA
SDS
Instruction de manipulation Technical Support

Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) binds to the target site on the dopamine transporter (DAT).

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CAS No. : 67469-78-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
5 mg En stock
10 mg En stock
25 mg En stock
50 mg En stock
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Based on 8 publication(s) in Google Scholar

Other Forms of Vanoxerine dihydrochloride:

Vanoxerine dihydrochloride Related Antibodies

Top Publications Citing Use of Products

    Vanoxerine dihydrochloride purchased from MedChemExpress. Usage Cited in: Nature. 2024 Aug;632(8025):686-694.  [Abstract]

    Concentration–inhibition curves of [3H]dopamine uptake by wild-type and indicated mutants of DAT with specified concentrations of GBR12909 (Vanoxerine dihydrochloride) in the range of 1 pM to 10 μM.

    Vanoxerine dihydrochloride 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.

    • Activité biologique

    • Pureté et documentation

    • Références

    • Avis client

    Description

    Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) binds to the target site on the dopamine transporter (DAT)[1].

    IC50 & Target

    Ki: 1 nM (dopamine reuptake)[1]
    In Vitro

    Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) inhibits the uptake of dopamlne (DA), with an IC50 in the low nanomolar range, and is several-fold less potent as inhibitors of the uptake of noradrenaline and 5-HT[2].
    Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is also an oral, mixed ion channel blocker with IKr, INa, and L-type calcium channel activity[3].

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

    Vanoxerine dihydrochloride Related Antibodies
    In Vivo

    Vanoxerine dihydrochloride (2.5-20 mg/kg; i.p.) significantly increases the ambulatory activity[3].

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

    Animal Model: Male mice (ddY strain at 6 weeks of age)[3]
    Dosage: 2.5, 5, 10, 20 mg/kg
    Administration: Intraperitoneal injection
    Result: The ambulatory activity of mice increased in a dose-dependent manner, with a maximal increase at 30 min after the administration.
    Masse moléculaire

    523.49

    Formule

    C28H34Cl2F2N2O
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    FC1=CC=C(C(C2=CC=C(F)C=C2)OCCN3CCN(CCCC4=CC=CC=C4)CC3)C=C1.[2HCl]
    Livraison

    Room temperature in continental US; may vary elsewhere.
    Stockage

    4°C, sealed storage, away from moisture

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

    Solvant et solubilité
    In Vitro: 

    DMSO : 9.4 mg/mL (17.96 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 1 mg/mL (1.91 mM; ultrasonic and warming and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9103 mL 9.5513 mL 19.1026 mL
    5 mM 0.3821 mL 1.9103 mL 3.8205 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.

    • Calculateur de molarité

    • Calculateur de dilution

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    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: ≥ 2.08 mg/mL (3.97 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (3.97 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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).

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

    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.
    Pureté et documentation

    Purity: 99.60%

    SDS (252 KB)

    COA (245 KB) LCMS (87 KB)

    Instruction de manipulation (2659 KB)
    Références

    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 1.9103 mL 9.5513 mL 19.1026 mL 47.7564 mL
    DMSO 5 mM 0.3821 mL 1.9103 mL 3.8205 mL 9.5513 mL
    10 mM 0.1910 mL 0.9551 mL 1.9103 mL 4.7756 mL
    15 mM 0.1274 mL 0.6368 mL 1.2735 mL 3.1838 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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    Vanoxerine dihydrochloride 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:

    Vanoxerine67469-78-7GBR-12909I893GBR12909GBR 12909I 893I-893Dopamine TransporterDATSLC6A3Inhibitorinhibitorinhibit

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