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Vilazodone Hydrochloride

Combined SSRI and 5-HT1A receptor partial agonist CAS# 163521-08-2

Vilazodone Hydrochloride

Catalog No. BCC2041----Order now to get a substantial discount!

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Quality Control of Vilazodone Hydrochloride

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Chemical structure

Vilazodone Hydrochloride

3D structure

Chemical Properties of Vilazodone Hydrochloride

Cas No. 163521-08-2 SDF Download SDF
PubChem ID 6918313 Appearance Powder
Formula C26H28ClN5O2 M.Wt 477.99
Type of Compound N/A Storage Desiccate at -20°C
Synonyms EMD 68843; SB659746A
Solubility DMSO : 25 mg/mL (52.30 mM; Need ultrasonic)
Chemical Name 5-[4-[4-(5-cyano-1H-indol-3-yl)butyl]piperazin-1-yl]-1-benzofuran-2-carboxamide;hydrochloride
SMILES C1CN(CCN1CCCCC2=CNC3=C2C=C(C=C3)C#N)C4=CC5=C(C=C4)OC(=C5)C(=O)N.Cl
Standard InChIKey RPZBRGFNBNQSOP-UHFFFAOYSA-N
Standard InChI InChI=1S/C26H27N5O2.ClH/c27-16-18-4-6-23-22(13-18)19(17-29-23)3-1-2-8-30-9-11-31(12-10-30)21-5-7-24-20(14-21)15-25(33-24)26(28)32;/h4-7,13-15,17,29H,1-3,8-12H2,(H2,28,32);1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Vilazodone Hydrochloride

DescriptionPotent 5-HT1A partial agonist and serotonin-selective reuptake inhibitor (SSRI) (IC50 values are 0.2 and 0.5 nM respectively). Antidepressant.

Vilazodone Hydrochloride Dilution Calculator

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Vilazodone Hydrochloride Molarity Calculator

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Preparing Stock Solutions of Vilazodone Hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.0921 mL 10.4605 mL 20.9209 mL 41.8419 mL 52.3023 mL
5 mM 0.4184 mL 2.0921 mL 4.1842 mL 8.3684 mL 10.4605 mL
10 mM 0.2092 mL 1.046 mL 2.0921 mL 4.1842 mL 5.2302 mL
50 mM 0.0418 mL 0.2092 mL 0.4184 mL 0.8368 mL 1.046 mL
100 mM 0.0209 mL 0.1046 mL 0.2092 mL 0.4184 mL 0.523 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Vilazodone Hydrochloride

Vilazodone (EMD 68843; SB 659746A; 5-{4-[4-(5-cyano-3-indolyl)-butyl]-1-piperazinyl}-benzofuran-2-carboxamide hydrochloride) is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist currently under clinical evaluation for the treatment of major depression.

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References on Vilazodone Hydrochloride

Development and Validation of a Stability-Indicating Liquid Chromatographic Method for Estimating Vilazodone Hydrochloride in Pharmaceutical Dosage Form Using Quality by Design.[Pubmed:27601040]

J Chromatogr Sci. 2016 Nov;54(10):1713-1722.

A stability-indicating liquid chromatographic method was developed employing the principles of quality by design (QbD) to quantify Vilazodone Hydrochloride (VLN) in pharmaceutical dosage form. A Box-Behnken experimental design was employed to establish optimum conditions including method robustness by selecting organic phase proportion (%), mobile phase flow rate (mL/min) and pH of buffer as the factors, to study their effect on plate number as the response variable. Chromatography was performed on a C-18 column using methanol:phosphate buffer of pH 7.0 (85:15, v/v) as the mobile phase at a flow rate of 1.2 mL/min with photo diode array (PDA) detection at 285 nm. Calibration curve was linear over 5-80 microg/mL with values of accuracy within 99.4-100.8%. The limit of detection and quantification were found to be 1.5 and 5.0 microg/mL, respectively. The developed method revealed high specificity for VLN and its degradation products formed during forced degradation conditions. Furthermore, control strategies were developed based on system suitability test result. The QbD-based developed liquid chromatographic method was found suitable for routine analysis of VLN in bulk drug and pharmaceutical dosage form.

Vilazodone hydrochloride, a combined SSRI and 5-HT1A receptor agonist for major depressive disorder.[Pubmed:23229074]

Consult Pharm. 2012 Dec;27(12):857-67.

OBJECTIVE: Vilazodone (VIIBRYD, Trovis Pharmaceuticals; New Haven, Connecticut, also known as 659746, EMD68843, SB-659746-A) is a newly introduced antidepressant that has taken approximately a decade from its discovery to approval by the Food and Drug Administration. This paper will review the chemistry, pharmacodynamics, pharmacokinetics, clinical efficacy, tolerability, drug-drug interaction potential, dosing, and administration of this agent. DATA SOURCES: Medline/PubMed/IPA/EMBASE databases were searched using the terms "vilazodone," "659746," "EMD68843," and "SB-659746-A." All English-language papers from 1985 to April 2012 were reviewed for relevance. Bibliographies of all papers were reviewed to identify further papers. STUDY SELECTION: All English-language papers from 1985 to present appearing in these searches were reviewed for relevance to this paper. In addition, their bibliographies were reviewed to identify any papers not identified in the searches. Data are expressed as mean or mean +/- standard deviation, unless otherwise noted. DATA SYNTHESIS: Vilazodone is the first combined selective serotonin reuptake inhibitor (SSRI)/5-HT1A receptor agonist antidepressant. Vilazodone must be administered with food to optimize bioavailability. The primary route of elimination is metabolism followed by excretion of metabolites. Advancing age and renal and hepatic impairment do not alter its disposition. Early phase II clinical trials were unable to demonstrate antidepressant efficacy. However, later phase III trials using 40 mg daily doses were able to demonstrate superior efficacy compared with placebo treatment. Adverse events, warnings, and precautions mirror those of other SSRIs. CONCLUSION: Although there are theoretical reasons why 5-HT1A agonism may be a desirable additional property in antidepressants, there is no evidence to date that vilazodone has any advantage over existing post-tricyclic antidepressants. It has a narrow therapeutic dosing range whose upper boundary is close to that producing intolerable gastrointestinal and central nervous system adverse events. Further research will clarify and refine the role of vilazodone in the management of psychiatric disorders.

Description

Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT1A receptor partial agonist.

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