Cat. No.: HY-14262

Vilazodone

(Synonyms: EMD 68843; SB659746A)

6 Cited Publications

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Based on 6 publication(s) in Google Scholar

Vilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active serotonin reuptake inhibitor (SSRI) and partial 5-HT₁A receptor agonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders.

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Pureté: 99.73%
CAS No.: 163521-12-8
Formule: C₂₆H₂₇N₅O₂
Masse moléculaire:441.52

Stockage:

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

Vilazodone Chemical Structure

CAS No.: 163521-12-8

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (6)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

5-HT_1A Receptor

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

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.2 nM Compound: 551	Agonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting method Agonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting method	[PMID: 29400967]
HEK293	EC₅₀	0.12 nM Compound: Vilazodone	Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay	[PMID: 30744931]

In Vitro

Vilazodone shows an IC₅₀ of 0.2 nM at the human 5-HT₁A receptor and 0.5 nM for the SERT. Vilazodone preferentially binds to the high agonist affinity state of human 5-HT₁A receptors, and it displays high affinity (pK_i≥9.3) for human recombinant and rat, guinea pig, mouse, and marmoset native tissue 5-HT_1A receptors.
Vilazodone acts as a high efficacy partial agonist at 5-HT₁A receptors. In [³⁵S]GTPγS binding studies in Sf9 cells expressing h5-HT₁A receptors, a single concentration of Vilazodone (100nM) increases basal binding by approximately 70% of that produced by the full 5-HT₁A receptor agonist, 8-OH-PIPAT.
In [³⁵S]GTPγS binding studies in rat hippocampal membranes, Vilazodone acts as a potent 5-HT_1A receptor partial agonist with a pEC₅₀ of 8.1 and an intrinsic activity of 0.61.
Vilazodone acts as a potent 5-HT reuptake inhibitor in rat and guinea pig cortex. In LLCPK cells expressing human SERT, whereby vilazodone inhibits [³H]5-HT uptake with a pIC₅₀ of 8.8^[1].

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

In Vivo

Vilazodone (intraperitoneal injection; 3 mg/kg ; single dose) produces increases in extracellular levels of 5-HT in both the frontal cortex (FC) and ventral hippocampus (vHipp) of rats in vivo microdialysis studies. Maximum increases are observed at 3 mg/kg and reaches 527% and 558% of preinjection baseline values in the FC and vHipp, respectively^[2].
Vilazodone (oral gavage ;55 mg/kg ; single dose) inhibits stress-induced vocalizations in the rat ultrasonic vocalizations test at 120 and 210 min post dose^[2].

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

Chemical Information

CAS No. 163521-12-8
Appearance Solid
Masse moléculaire 441.52
Formule C₂₆H₂₇N₅O₂
Color White to light yellow
SMILES

NC(C1=CC2=C(C=CC(N3CCN(CCCCC4=CNC5=CC=C(C=C54)C#N)CC3)=C2)O1)=O
Synonyms

EMD 68843; SB659746A
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (6)

All In Vivo Efficacy StudyHistological Imaging/StainingIHCELISA

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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
Cell

Unveiling conformation-selective regulation of the norepinephrine transporter. [Abstract]

2025 Nov 26;188(24):6861-6872.e14. PMID: 41138730
Adv Sci (Weinh)

Macrophage TRIM21 Inhibition Ameliorates Murine Acute Pancreatitis via PHB2-Mediated Mitochondrial Stabilization. [Abstract]

2026 Jan 22:e17877. PMID: 41572443

Vilazodone purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2026 Jan 22:e17877. [Abstract]

Vilazodone(25 mg/kg, i.p.)-treated mice exhibited pronounced pancreatic edema and increased pancreas‐to‐body weight ratios.

Vilazodone purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2026 Jan 22:e17877. [Abstract]

H&E staining indicated that Vilazodone (25 mg/kg, i.p.) significantly exacerbated pancreatic injury in L-arginine-treated AP mice compared to controls.

Vilazodone purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2026 Jan 22:e17877. [Abstract]

IHC confirmed aggravated local and systemic inflammation, evidenced by increased levels of IL‐1β and TNF-α in Vilazodone (25 mg/kg, i.p.)-treated mice with AP.

Vilazodone purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2026 Jan 22:e17877. [Abstract]

ELISA confirmed aggravated local and systemic inflammation, evidenced by increased levels of IL‐1β and TNF‐α in Vilazodone (25 mg/kg, i.p.)‐treated mice with AP.
Prog Neuropsychopharmacol Biol Psychiatry

A critical step in antidepressants onset: Excitation of glutamatergic pyramidal neurons in rodents' medial prefrontal cortex. [Abstract]

2024 Mar 2:130:110911. PMID: 38065287
Arch Pharm (Weinheim)

Identification of vilazodone as a novel plasminogen activator inhibitor to overcome Alzheimer's disease through virtual screening, molecular dynamics simulation, and biological evaluation. [Abstract]

2024 May 30:e2400263. PMID: 38816779
Mol Pharmacol

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

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

Solvant et solubilité

In Vitro:

DMSO : 75 mg/mL (169.87 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

2.2649 mL

11.3245 mL

22.6490 mL

5 mM

0.4530 mL

2.2649 mL

4.5298 mL

10 mM

0.2265 mL

1.1325 mL

2.2649 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.

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 (5.66 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% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.66 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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (275 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)
Instruction de manipulation (2659 KB)

Références

[1]. Lee A. Dawson et al. Vilazodone: A 5-HT1A Receptor Agonist/Serotonin Transporter Inhibitor for the Treatment of Affective Disorders CNS Neuroscience & Therapeutics Volume 15, Issue 2, pages 107-117, June 2009

[2]. Cruz MP. Vilazodone HCl (Viibryd): A Serotonin Partial Agonist and Reuptake Inhibitor For the Treatment of Major Depressive Disorder. P T. 2012 Jan;37(1):28-31. [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	2.2649 mL	11.3245 mL	22.6490 mL	56.6226 mL
	5 mM	0.4530 mL	2.2649 mL	4.5298 mL	11.3245 mL
	10 mM	0.2265 mL	1.1325 mL	2.2649 mL	5.6623 mL
	15 mM	0.1510 mL	0.7550 mL	1.5099 mL	3.7748 mL
	20 mM	0.1132 mL	0.5662 mL	1.1325 mL	2.8311 mL
	25 mM	0.0906 mL	0.4530 mL	0.9060 mL	2.2649 mL
	30 mM	0.0755 mL	0.3775 mL	0.7550 mL	1.8874 mL
	40 mM	0.0566 mL	0.2831 mL	0.5662 mL	1.4156 mL
	50 mM	0.0453 mL	0.2265 mL	0.4530 mL	1.1325 mL
	60 mM	0.0377 mL	0.1887 mL	0.3775 mL	0.9437 mL
	80 mM	0.0283 mL	0.1416 mL	0.2831 mL	0.7078 mL
	100 mM	0.0226 mL	0.1132 mL	0.2265 mL	0.5662 mL

Keywords

Vilazodone

6 Cited Publications

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Vilazodone

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Publications Citing Use of MedChemExpress (MCE) Vilazodone

Voir tous les produits spécifiques à Isoform 5-HT Receptor

Activité biologique

Chemical Information

Publications (6)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Vilazodone Related Classifications

HY-14262 Related Classifications