2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor Serotonin Transporter
  4. Vilazodone

Vilazodone  (Synonyms: EMD 68843; SB659746A)

Cat. No.: HY-14262 Purity: 99.84%
COA Handling Instructions

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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.

For research use only. We do not sell to patients.

Vilazodone Chemical Structure

Vilazodone Chemical Structure

CAS No. : 163521-12-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 262 In-stock
Solution
10 mM * 1 mL in DMSO USD 262 In-stock
Solid
5 mg USD 153 In-stock
10 mg USD 238 In-stock
50 mg USD 396 In-stock
100 mg   Get quote  
200 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Vilazodone:

Vilazodone Related Antibodies

Top Publications Citing Use of Products

View All 5-HT Receptor Isoform Specific Products:

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2].

IC50 & Target

5-HT1A Receptor

 

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 (pKi≥9.3) for human recombinant and rat, guinea pig, mouse, and marmoset native tissue 5-HT1A 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‐HT1A 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.

Vilazodone Related Antibodies
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.
Clinical Trial
Molecular Weight

441.52

Formula

C26H27N5O2
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2649 mL 11.3245 mL 22.6490 mL
5 mM 0.4530 mL 2.2649 mL 4.5298 mL
View the Complete Stock Solution Preparation Table

* 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.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.84%

COA (249 KB) RP-HPLC (326 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

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
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Vilazodone Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Vilazodone163521-12-8EMD 68843 SB659746AEMD68843EMD-688435-HT ReceptorSerotonin TransporterSerotonin Receptor5-hydroxytryptamine Receptor5-HTTSERTSLC6A4major depressive disorderMDDAffective DisorderInhibitorinhibitorinhibit

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