Cat. No.: HY-15414A

Vortioxetine hydrobromide

(Synonyms: Lu AA21004 hydrobromide)

11 Cited Publications

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Based on 11 publication(s) in Google Scholar

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

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Pureté: 99.87%
CAS No.: 960203-27-4
Formule: C₁₈H₂₃BrN₂S
Masse moléculaire:379.36

Stockage:

4°C, sealed storage, away from moisture

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

Vortioxetine hydrobromide Chemical Structure

CAS No.: 960203-27-4

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Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (11)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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)

5-HT₇ Receptor

19 nM (Ki)

SERT

1.6 nM (Ki)

Voir tous les produits spécifiques à Isoform 5-HT Receptor :

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 960203-27-4
Appearance Solid
Masse moléculaire 379.36
Formule C₁₈H₂₃BrN₂S
Color Light yellow to yellow
SMILES

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

Lu AA21004 hydrobromide
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)

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 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).
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

Solvant et solubilité

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)

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

2.6360 mL

13.1801 mL

26.3602 mL

5 mM

0.5272 mL

2.6360 mL

5.2720 mL

10 mM

0.2636 mL

1.3180 mL

2.6360 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, 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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 (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.

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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (6.59 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
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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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (279 KB)
SDS (393 KB)
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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)
Instruction de manipulation (2659 KB)

Références

[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]. Mork 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

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

Keywords

Vortioxetine hydrobromide

11 Cited Publications

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Vortioxetine hydrobromide

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Publications Citing Use of MedChemExpress (MCE) Vortioxetine hydrobromide

Voir tous les produits spécifiques à Isoform 5-HT Receptor

Activité biologique

Chemical Information

Publications (11)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Vortioxetine hydrobromide Related Classifications

HY-15414A Related Classifications