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Vortioxetine

Catalog No.GC16312 Copy One-Click Copy Product Info

Vortioxetine is a multimodal antidepressant, with high affinity for recombinant human 5-HT1A (Ki=15nM), 5-HT1B (Ki=33nM), 5-HT3A (Ki=3.7nM), 5-HT7 (Ki=19nM), and noradrenergic β1 receptor (Ki=46nM), and SERT (Ki=1.6nM).

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Vortioxetine Chemical Structure

Cas No.: 508233-74-7

Size Price Stock Qty
10mM (in 1mL DMSO)
$39.00
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5mg
$22.00
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10mg
$35.00
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50mg
$77.00
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100mg
$105.00
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200mg
$173.00
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500mg
$315.00
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Sample solution is provided at 25 µL, 10mM.



Description of Vortioxetine

Vortioxetine is a multimodal antidepressant, with high affinity for recombinant human 5-HT1A (Ki=15nM), 5-HT1B (Ki=33nM), 5-HT3A (Ki=3.7nM), 5-HT7 (Ki=19nM), and noradrenergic β1 receptor (Ki=46nM), and SERT (Ki=1.6nM)[1]. Vortioxetine exerts the antidepressant effect by regulating the activity of 5-hydroxytryptamine receptors and inhibiting the 5-hydroxytryptamine transporter [2]. Vortioxetine has been widely used in various animal models to improve cognitive abilities and the ability to recognize new objects[3].

In vitro, Vortioxetine treatment for 24 hours significantly inhibited the growth of AGS cells with an IC50 value of 25.1µM [4]. Treatment of A172 cells with 4μM Vortioxetine for 48h decreased the migration ability of A172 cells, decreased the expression levels of N-cadherin and Slug, and increased the expression levels of E-cadherin[5].

In vivo, Vortioxetine, administered orally at a dose of 10mg/kg daily for 3 weeks, improved context discrimination (CD) in GFAP-TK+ mouse models[6]. Daily intraperitoneal injection of Vortioxetine at a dose of 10mg/kg/day for 4 weeks reversed the reduction in anxiety-like behavior and ameliorated impairments in recognition and spatial reference memory in 5×FAD mice[7]. Daily subcutaneous injection of Vortioxetine at a dose of 10mg/kg for two weeks significantly improved levodopa-induced dyskinesia in mice[8].

References:
[1] Bang-Andersen B, Ruhland T, Jørgensen M, et al. Discovery of 1-[2-(2, 4-dimethylphenylsulfanyl) phenyl] piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder[J]. Journal of medicinal chemistry, 2011, 54(9): 3206-3221.
[2] Chen G, Højer A M, Areberg J, et al. Vortioxetine: clinical pharmacokinetics and drug interactions[J]. Clinical Pharmacokinetics, 2018, 57(6): 673-686.
[3] Sanchez C, Asin K E, Artigas F. Vortioxetine, a novel antidepressant with multimodal activity: review of preclinical and clinical data[J]. Pharmacology & therapeutics, 2015, 145: 43-57.
[4] Lv G B, Wang T T, Zhu H L, et al. Vortioxetine induces apoptosis and autophagy of gastric cancer AGS cells via the PI3K/AKT pathway[J]. FEBS open bio, 2020, 10(10): 2157-2165.
[5] Zhang H, Zhang D, Huang Z, et al. Vortioxetine exhibits anti-glioblastoma activity via the PI3K-Akt signaling pathway[J]. Iranian Journal of Basic Medical Sciences, 2025, 28(4): 401.
[6] Felice D, Guilloux J P, Pehrson A, et al. Vortioxetine improves context discrimination in mice through a neurogenesis independent mechanism[J]. Frontiers in pharmacology, 2018, 9: 204.
[7] Jiang L X, Huang G D, Su F, et al. Vortioxetine administration attenuates cognitive and synaptic deficits in 5× FAD mice[J]. Psychopharmacology, 2020, 237(4): 1233-1243.
[8] Budrow C, Elder K, Coyle M, et al. Broad serotonergic actions of vortioxetine as a promising avenue for the treatment of L-DOPA-induced dyskinesia[J]. Cells, 2023, 12(6): 837.

Protocol of Vortioxetine

Cell experiment [1]:

Cell lines

A172 cells

Preparation Method

A172 cells were cultured in high-glucose DMEM medium supplemented with 10% fetal bovine serum (FBS), 100U/ml penicillin, and 100μg/ml streptomycin in a humidified incubator at 37℃ with 5% CO2. Cells were seeded in 96-well plates at a density of 4×103 cells per well and allowed to adhere overnight before being treated with various concentrations of Vortioxetine (0, 2, 4, 6, 8, and 10µM) for 72h and cell viability was analyzed.

Reaction Conditions

0, 2, 4, 6, 8, and 10µM; 72h

Applications

Vortioxetine treatment reduced the cell viability of A172 cells in a dose-dependent manner.
Animal experiment [2]:

Animal models

5×FAD mice

Preparation Method

5×FAD mice were maintained in a temperature and relative humidity-controlled environment (22±2°C, 40 to 70%) with a light/dark cycle of 12h/12h. Food and water were available ad libitum. The mice were divided into two groups: the experimental group was treated with Vortioxetine at a dose of 10mg/kg daily intraperitoneally for 4 weeks; the control group received normal saline without Vortioxetine. After 4 weeks of administration, behavioral tests were performed.

Dosage form

10mg/kg/day for 4 weeks; i.p.

Applications

Vortioxetine treatment improved the impairment in recognition memory function in the 5×FAD mice.

References:
[1] Zhang H, Zhang D, Huang Z, et al. Vortioxetine exhibits anti-glioblastoma activity via the PI3K-Akt signaling pathway[J]. Iranian Journal of Basic Medical Sciences, 2025, 28(4): 401.
[2] Jiang L X, Huang G D, Su F, et al. Vortioxetine administration attenuates cognitive and synaptic deficits in 5× FAD mice[J]. Psychopharmacology, 2020, 237(4): 1233-1243.

Chemical Properties of Vortioxetine

Cas No. 508233-74-7 SDF
Chemical Name 1-[2-(2,4-dimethylphenyl)sulfanylphenyl]piperazine
Canonical SMILES CC1=CC(=C(C=C1)SC2=CC=CC=C2N3CCNCC3)C
Formula C18H22N2S M.Wt 298.45
Solubility ≥ 14.9 mg/mL in DMSO, ≥ 4.31 mg/mL in EtOH with ultrasonic Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Vortioxetine

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 3.3506 mL 16.7532 mL 33.5064 mL
5 mM 670.1 μL 3.3506 mL 6.7013 mL
10 mM 335.1 μL 1.6753 mL 3.3506 mL
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In vivo Formulation Calculator (Clear solution) of Vortioxetine

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Review for Vortioxetine

Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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