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Vilazodone
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Catalog No. T1279Cas No. 163521-12-8
Alias SB659746A, EMD 68843
Vilazodone (SB659746A) is a selective serotonin (5-HT) reuptake inhibitor (SSRI) and a 5-HT-1A receptor partial agonist, with antidepressant and anti-anxiety activities. Vilazodone inhibits the reuptake of serotonin from the synaptic cleft while stimulating the release of 5-HT into the synaptic cleft. This increases the concentration of 5-HT in the synaptic cleft and potentiates serotonergic neurotransmission in the central nervous system.
Vilazodone
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Purity: 99.61%
Catalog No. T1279Alias SB659746A, EMD 68843Cas No. 163521-12-8
Vilazodone (SB659746A) is a selective serotonin (5-HT) reuptake inhibitor (SSRI) and a 5-HT-1A receptor partial agonist, with antidepressant and anti-anxiety activities. Vilazodone inhibits the reuptake of serotonin from the synaptic cleft while stimulating the release of 5-HT into the synaptic cleft. This increases the concentration of 5-HT in the synaptic cleft and potentiates serotonergic neurotransmission in the central nervous system.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $54 | In Stock | In Stock | |
| 5 mg | $127 | In Stock | In Stock | |
| 10 mg | $197 | In Stock | In Stock | |
| 25 mg | $278 | In Stock | In Stock | |
| 50 mg | $329 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $154 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.61%
Appearance:Solid
Color:White
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Product Introduction
Vilazodone AI Summary
Vilazodone exhibits potent bioactivities related to serotonin regulation and has demonstrated interactions with various neurotransmitter systems. It has a high affinity for the human 5-HT1A receptor (Ki = 0.2 nM) and exhibits agonist activity at this receptor with an EC50 value of 0.12 nM. The compound effectively inhibits the serotonin transporter (SERT) with an IC50 value ranging from 0.4 to 0.5 nM, indicating its potential to modulate serotonin levels. Additionally, it shows inhibitory activity against the dopamine receptors (D2, D3, D4), adrenergic receptors (alpha-1, alpha-2), histamine H1 receptor, and rat cortex acetylcholinesterase (AChE) with an IC50 of 21300.0 nM.
In antiviral assays, Vilazodone displays activity against SARS-CoV-2 with modest inhibition rates, including a hit score of 0.1122 in HRCE cells and a 0.71% inhibition rate of SARS-CoV-2 induced cytotoxicity in VERO-6 cells. It also inhibits the SARS-CoV-2 3CL-Pro protease by approximately 9.82% at 20 µM.
Metabolic stability of Vilazodone is moderate to low in liver microsomes, with half-lives around 0.4-0.474 hours in rat, mouse, and human models. These findings, combined with good permeability in PAMPA-BBB assays and moderate inhibition of several cytochrome P450 enzymes, suggest potential challenges in drug-drug interactions and systemic exposure.
The compound also demonstrates antidepressant properties in mice, reducing immobility time by 60% at a dose of 40 mg/kg for 7 days. It exhibits cytotoxicity in human HepG2 cells with an IC50 value of 6100.0 nM.
Overall, Vilazodone is a promising serotonin modulator with potential therapeutic implications in serotonin-related disorders, although further research is needed to address its metabolic stability and broad receptor interactions..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Vilazodone (SB659746A) is a selective serotonin (5-HT) reuptake inhibitor (SSRI) and a 5-HT-1A receptor partial agonist, with antidepressant and anti-anxiety activities. Vilazodone inhibits the reuptake of serotonin from the synaptic cleft while stimulating the release of 5-HT into the synaptic cleft. This increases the concentration of 5-HT in the synaptic cleft and potentiates serotonergic neurotransmission in the central nervous system. |
| Synonyms | SB659746A, EMD 68843 |
| Molecular Weight | 441.52 |
| Formula | C26H27N5O2 |
| Cas No. | 163521-12-8 |
| Smiles | NC(=O)c1cc2cc(ccc2o1)N1CCN(CCCCc2c[nH]c3ccc(cc23)C#N)CC1 |
| Relative Density. | 1.34 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 68.57 mg/mL (155.3 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.53 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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