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

Vortioxetine  (Synonyms: Lu AA 21004)

製品番号: HY-15414 純度: 98.61%
COA 取扱説明書 Technical Support

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

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CAS 番号 : 508233-74-7

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 38 在庫あり
Solution
10 mM * 1 mL in DMSO USD 38 在庫あり
Solid
5 mg $35 在庫あり
10 mg $55 在庫あり
25 mg $90 在庫あり
50 mg $121 在庫あり
100 mg $165 在庫あり
200 mg $275 在庫あり
500 mg $495 在庫あり
1 g $715 在庫あり
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カスタマーレビュー

Based on 10 publication(s) in Google Scholar

Other Forms of Vortioxetine:

Vortioxetine 関連抗体

Top Publications Citing Use of Products

    Vortioxetine 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 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 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).

    5-HT Receptor アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

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    • 純度とドキュメンテーション

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    製品説明

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

    Human 5-HT7 Receptor

    19 nM (Ki)

    SERT

    1.6 nM (Ki)

    Cellular Effect
    Cell Line Type Value Description References
    Monocyte IC50
    2.9 nM
    Compound: 1
    Inhibition of PMA-induced oxidative burst in human monocytes preincubated for 1 hr followed by PMA stimulation and measured after 30 mins
    Inhibition of PMA-induced oxidative burst in human monocytes preincubated for 1 hr followed by PMA stimulation and measured after 30 mins
    		[PMID: 32992247]
    体外実験

    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 関連抗体
    体内実験

    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.
    分子量

    298.45

    分子式

    C18H22N2S
    CAS 番号
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    CC1=CC=C(SC2=CC=CC=C2N3CCNCC3)C(C)=C1
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 50 mg/mL (167.53 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 3.3506 mL 16.7532 mL 33.5064 mL
    5 mM 0.6701 mL 3.3506 mL 6.7013 mL
    10 mM 0.3351 mL 1.6753 mL 3.3506 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

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    体内:

    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 (8.38 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 (8.38 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      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
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    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.
    純度とドキュメンテーション
    参考文献

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.3506 mL 16.7532 mL 33.5064 mL 83.7661 mL
    5 mM 0.6701 mL 3.3506 mL 6.7013 mL 16.7532 mL
    10 mM 0.3351 mL 1.6753 mL 3.3506 mL 8.3766 mL
    15 mM 0.2234 mL 1.1169 mL 2.2338 mL 5.5844 mL
    20 mM 0.1675 mL 0.8377 mL 1.6753 mL 4.1883 mL
    25 mM 0.1340 mL 0.6701 mL 1.3403 mL 3.3506 mL
    30 mM 0.1117 mL 0.5584 mL 1.1169 mL 2.7922 mL
    40 mM 0.0838 mL 0.4188 mL 0.8377 mL 2.0942 mL
    50 mM 0.0670 mL 0.3351 mL 0.6701 mL 1.6753 mL
    60 mM 0.0558 mL 0.2792 mL 0.5584 mL 1.3961 mL
    80 mM 0.0419 mL 0.2094 mL 0.4188 mL 1.0471 mL
    100 mM 0.0335 mL 0.1675 mL 0.3351 mL 0.8377 mL
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    Vortioxetine Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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:

    Vortioxetine508233-74-7Lu AA 21004Lu AA21004Lu AA-210045-HT ReceptorSerotonin TransporterSerotonin Receptor5-hydroxytryptamine Receptor5-HTTSERTSLC6A4Inhibitorinhibitorinhibit

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    製品名:
    Vortioxetine
    製品番号:
    HY-15414
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