2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor Serotonin Transporter
  4. Vortioxetine hydrobromide

Vortioxetine hydrobromide  (Synonyms: Lu AA21004 hydrobromide)

Cat. No.: HY-15414A Purity: 99.87%
COA
SDS
Handling Instructions Technical Support

Vortioxetine (Lu AA 21004) hydrobromide is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM).

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

CAS No. : 960203-27-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Vortioxetine hydrobromide:

Vortioxetine hydrobromide Related Antibodies

Top Publications Citing Use of Products

    Vortioxetine hydrobromide purchased from MedChemExpress. Usage Cited in: Biomedicines. 2022 Jun 3;10(6):1318.  [Abstract]

    Representative current traces acquired in the absence (upper) and presence (lower) of 10 μM VOR. Voltage-clamp protocol that we used is illustrated in the uppermost part.

    Vortioxetine hydrobromide purchased from MedChemExpress. Usage Cited in: Biomedicines. 2022 Jun 3;10(6):1318.  [Abstract]

    Representative current traces obtained in the presence of 10 μM Vortioxetine (upper) and 30 μM Vortioxetine (lower). The uppermost parts denote the voltage-clamp protocol applied. The right side shows the expanded records (i.e., potential and current traces) taken from the dashed box in the left side for a short time scale.

    Vortioxetine hydrobromide purchased from MedChemExpress. Usage Cited in: Biomedicines. 2022 Jun 3;10(6):1318.  [Abstract]

    The mean relationship of the relative amplitude versus the interpulse interval in the absence (filled gray squares) and presence of 10 mM Vortioxetine (open blue squares) or 30 μM Vortioxetine (open red circles). The x-axis is displayed on the logarithmic scale. The time course as indicated in smooth line was goodness-of-fit to a single exponential. Each point represents the mean ± SEM (n = 7).

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    5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Vortioxetine (Lu AA 21004) hydrobromide is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM)[1][2].

    IC50 & Target

    5-HT1A Receptor

     

    5-HT1B Receptor

     

    5-HT3A Receptor

     

    5-HT7 Receptor

     

    sPLA2

    15 nM (Ki)

    5-HT3A Receptor

    3.7 nM (Ki)

    5-HT7 Receptor

    19 nM (Ki)

    SERT

    1.6 nM (Ki)

    In Vitro

    Vortioxetine (Compound 5m) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively. Vortioxetine displays antagonistic properties at 5-HT3A and 5-HT7 receptors, partial agonist properties at 5-HT1B receptors, agonistic properties at 5-HT1A receptors, and potent inhibition of SERT[1]. Vortioxetine is a partial h5-HT 1B receptor agonist with EC50 of 460 nM and intrinsic activity of 22% using a whole-cell cAMP-based assay. Vortioxetine binds to the r5-HT 7 receptor with a Ki value of 200 nM and is a functional antagonist at the r5-HT7 receptor with an IC50 of 2 μM in an in vitro whole-cell cAMP assay[5].

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

    Vortioxetine hydrobromide Related Antibodies
    In Vivo

    Vortioxetine (Lu AA21004) occupies the r5-HT1B receptor and rSERT (ED50= 3.2 and 0.4 mg/kg, respectively) after subcutaneous administration and is a 5-HT3 receptor antagonist[6]. Vortioxetine significantly increases cell proliferation and cell survival and stimulates maturation of immature granule cells in the sub granular zone of the dentate gyrus of the hippocampus after 21 days of treatment[3]. Vortioxetine does not cause cognitive or psychomotor impairment[4].

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

    379.36

    Formula

    C18H23BrN2S
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    CC1=CC=C(SC2=CC=CC=C2N3CCNCC3)C(C)=C1.[H]Br
    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: 

    DMSO : 25 mg/mL (65.90 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 2.6360 mL 13.1801 mL 26.3602 mL
    5 mM 0.5272 mL 2.6360 mL 5.2720 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.

    • 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: ≥ 2.5 mg/mL (6.59 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 (6.59 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).

    *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.
    Purity & Documentation

    Purity: 99.87%

    SDS (393 KB)

    COA (252 KB) RP-HPLC (264 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 (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
    DMSO 1 mM 2.6360 mL 13.1801 mL 26.3602 mL 65.9005 mL
    5 mM 0.5272 mL 2.6360 mL 5.2720 mL 13.1801 mL
    10 mM 0.2636 mL 1.3180 mL 2.6360 mL 6.5900 mL
    15 mM 0.1757 mL 0.8787 mL 1.7573 mL 4.3934 mL
    20 mM 0.1318 mL 0.6590 mL 1.3180 mL 3.2950 mL
    25 mM 0.1054 mL 0.5272 mL 1.0544 mL 2.6360 mL
    30 mM 0.0879 mL 0.4393 mL 0.8787 mL 2.1967 mL
    40 mM 0.0659 mL 0.3295 mL 0.6590 mL 1.6475 mL
    50 mM 0.0527 mL 0.2636 mL 0.5272 mL 1.3180 mL
    60 mM 0.0439 mL 0.2197 mL 0.4393 mL 1.0983 mL
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    Vortioxetine hydrobromide 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:

    Vortioxetine960203-27-4Lu AA21004Lu AA 21004Lu AA-210045-HT ReceptorSerotonin TransporterSerotonin Receptor5-hydroxytryptamine Receptor5-HTTSERTSLC6A4Inhibitorinhibitorinhibit

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