Referencia número: HY-15414

Vortioxetine

(Synonyms: Lu AA 21004)

11 Cited Publications

Revisión del cliente

Based on 11 publication(s) in Google Scholar

Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT_1A agonist and a partial agonist of 5-HT_1B (K_i: 15 nM, 33 nM).

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Pureza: 98.61%
No. CAS: 508233-74-7
Fòrmula: C₁₈H₂₂N₂S
Peso molecular:298.45

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Vortioxetine Chemical Structure

No. CAS: 508233-74-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (11)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

5-HT_1A Receptor

5-HT_1B Receptor

5-HT_3A Receptor

5-HT₇ Receptor

sPLA2

15 nM (Ki)

5-HT_3A Receptor

3.7 nM (Ki)

Human 5-HT₇ Receptor

19 nM (Ki)

SERT

1.6 nM (Ki)

Ver todos los productos específicos de isoformas 5-HT Receptor :

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]

In Vitro

Vortioxetine (Compound 5m) is a multimodal serotonergic agent, inhibits 5-HT_1A, 5-HT_1B, 5-HT_3A, 5-HT₇ receptor and SERT with K_i values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively. Vortioxetine displays antagonistic properties at 5-HT_3A and 5-HT₇ receptors, partial agonist properties at 5-HT_1B receptors, agonistic properties at 5-HT_1A 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-HT₇ receptor with a K_i 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.

In Vivo

Vortioxetine (Lu AA21004) occupies the r5-HT_1B 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.

Chemical Information

No. CAS 508233-74-7
Appearance Solid
Peso molecular 298.45
Fòrmula C₁₈H₂₂N₂S
Color Light yellow to yellow
SMILES

CC1=CC=C(SC2=CC=CC=C2N3CCNCC3)C(C)=C1
Synonyms

Lu AA 21004
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (11)

All Bio/Physico-chemical Assay

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Journal Impact Factor

Nature

Ligand recognition and G protein coupling of trace amine receptor TAAR1. [Abstract]

2023 Dec;624(7992):672-681. PMID: 37935376
Antioxidants (Basel)

Pitavastatin Calcium Confers Fungicidal Properties to Fluconazole by Inhibiting Ubiquinone Biosynthesis and Generating Reactive Oxygen Species. [Abstract]

2024 May 29;13(6):667. PMID: 38929106
Neurobiol Dis

Glial expression of Drosophila UBE3A causes spontaneous seizures that can be modulated by 5-HT signaling. [Abstract]

2024 Oct 1:200:106651. PMID: 39197537
Eur J Pharmacol

Mechanisms of NMDA receptor inhibition by vortioxetine - Comparison with fluoxetine. [Abstract]

2025 Jul 5:998:177460. PMID: 40049576
Psychiatry Res

The role of reelin in the pathological mechanism of depression from clinical to rodents. [Abstract]

2022 Nov:317:114838. PMID: 36103758
Biomedicines

Inhibitory Effectiveness in Delayed-Rectifier Potassium Current Caused by Vortioxetine, Known to Be a Novel Antidepressant. [Abstract]

2022 Jun 3;10(6):1318. PMID: 35740340

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).
Eur Arch Psychiatry Clin Neurosci

YY1 (Yin-Yang 1), a transcription factor regulating systemic inflammation, is involved in cognitive impairment of depression. [Abstract]

2023 Mar;77(3):149-159. PMID: 36436207
Mol Pharmacol

G α Protein Signaling Bias at Serotonin 1A Receptor. [Abstract]

2023 Nov;104(5):230-238. PMID: 37567783
Pharmacol Res Perspect

Comparative Sleep Architecture Profiles of Antidepressants in Mice: Pharmacological Characterization of Paroxetine, Sertraline, Duloxetine, Mirtazapine and Vortioxetine. [Abstract]

2026 Jun;14(3):e70246. PMID: 42083131
bioRxiv

2025 February 08.
bioRxiv

Glial expression of Drosophila UBE3A causes spontaneous seizures modulated by 5-HT signaling. [Abstract]

2024 Feb 9:2024.02.08.579543. PMID: 38370819

Solvente y solubilidad

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (8.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Bang-Andersen B, 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 Med Chem. 2011 May 12;54(9):3206-21. [Content Brief]

[2]. Guilloux JP, et al. Antidepressant and anxiolytic potential of the multimodal antidepressant vortioxetine (Lu AA21004) assessed by behavioural and neurogenesis outcomes in mice. Neuropharmacology. 2013 May 28;73C:147-159. [Content Brief]

[3]. Theunissen EL, et al. A randomized trial on the acute and steady-state effects of a new antidepressant, vortioxetine (Lu AA21004), on actual driving and cognition. Clin Pharmacol Ther. 2013 Jun;93(6):493-501. [Content Brief]

[4]. Rothschild AJ, et al. Vortioxetine (Lu AA21004) 5mg in generalized anxiety disorder: results of an 8-week randomized, double-blind, placebo-controlled clinical trial in the United States. Eur Neuropsychopharmacol. 2012 Dec;22(12):858-66. [Content Brief]

[5]. Mrk A, et al. Pharmacological effects of Lu AA21004: a novel multimodal compound for the treatment of major depressive disorder. J Pharmacol Exp Ther. 2012 Mar;340(3):666-75. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Vortioxetine

11 Cited Publications

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Vortioxetine

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Publications Citing Use of MedChemExpress (MCE) Vortioxetine

Ver todos los productos específicos de isoformas 5-HT Receptor

Actividad biológica

Chemical Information

Publications (11)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Vortioxetine Related Classifications

HY-15414 Related Classifications