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

Vilazodone (Synonyms: EMD 68843; SB659746A)

Cat. No.: HY-14262 Purity: 99.91%
Handling Instructions

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

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Solution
10 mM * 1 mL in DMSO USD 262 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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Estimated Time of Arrival: December 31
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10 mg USD 238 In-stock
Estimated Time of Arrival: December 31
50 mg USD 396 In-stock
Estimated Time of Arrival: December 31
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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].

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].

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.
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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (226.49 mM)

*"≥" means soluble, but saturation unknown.

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
10 mM 0.2265 mL 1.1325 mL 2.2649 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.91%

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Keywords:

VilazodoneEMD 68843 SB659746AEMD68843EMD-688435-HT ReceptorSerotonin TransporterSerotonin Receptor5-hydroxytryptamine Receptor5-HTTSERTSLC6A4major depressive disorderMDDAffective DisorderInhibitorinhibitorinhibit

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