Desvenlafaxine Succinate

Catalog No.S4112 Synonyms: WY 45233 Succinate

For research use only.

Desvenlafaxine Succinate (WY 45233) is a new serotonin (5-HT) transporter and norepinephrine (NE) transporter reuptake inhibitor with Ki of 40.2 nM and 558.4 nM respectively.

Desvenlafaxine Succinate Chemical Structure

CAS No. 386750-22-7

Selleck's Desvenlafaxine Succinate has been cited by 1 Publication

Purity & Quality Control

Choose Selective Serotonin Transporter Inhibitors

Biological Activity

Description Desvenlafaxine Succinate (WY 45233) is a new serotonin (5-HT) transporter and norepinephrine (NE) transporter reuptake inhibitor with Ki of 40.2 nM and 558.4 nM respectively.
Features A major active metabolite of venlafaxine.
Targets
5-HT [1] Norepinephrine (NE) [1]
40.2 nM(Ki) 558.4 nM(Ki)
In vitro

Desvenlafaxine succinate is the succinate salt monohydrate of O-desmethylvenlafaxine, an active metabolite of venlafaxine. Desvenlafaxine Succinate is a serotonin-norepinephrine reuptake inhibitor and is the active metabolite of the antidepressant venlafaxine. Similar to venlafaxine, Desvenlafaxine Succinate inhibits the neuronal uptake of serotonin and norepinephrine. Desvenlafaxine Succinate shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter. Desvenlafaxine Succinate inhibits [3H]5-HT or [3H]NE uptake for the hSERT or hNET with IC50 of 47.3 and 531.3 nM, respectively.[1] Desvenlafaxine Succinate has the potential to inhibit CYP2D6, which could result in increased concentrations of drugs metabolized through this pathway. Induction of CYP3A4 is also possible with Desvenlafaxine Succinate, which could impact the metabolism of drugs metabolized via this enzyme. [2]

In vivo Desvenlafaxine Succinate rapidly penetrates the male rat brain and hypothalamus. Desvenlafaxine Succinate significantly increases extracellular NE levels compared with baseline in the male rat hypothalamus but had no effect on DA levels using microdialysis. [1] Desvenlafaxine Succinate exhibits a linear and dose-proportional pharmacokinetic single-dose profile in a dose range from 100 to 600 mg/day. The absolute bioavailability of the oral formulation is 80.5%.[2]

Protocol (from reference)

Animal Research:[1]
  • Animal Models: Male Sprague-Dawley rats
  • Dosages: 30 mg/kg
  • Administration: Oral

Solubility (25°C)

In vitro

DMSO 80 mg/mL
(191.22 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
0.5% methylcellulose+0.2% Tween 80
For best results, use promptly after mixing.

30 mg/mL

Chemical Information

Molecular Weight 418.36
Formula

C22H24ClN3O.HCl

CAS No. 386750-22-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN(C)CC(C1=CC=C(C=C1)O)C2(CCCCC2)O.C(CC(=O)O)C(=O)O.O

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02637193 Completed Drug: Venlafaxine|Drug: Moxifloxacin|Drug: Drug - placebo Healthy Subjects Pfizer''s Upjohn has merged with Mylan to form Viatris Inc.|Pfizer December 2015 Phase 1
NCT02200406 Completed Drug: Desvenlafaxine Depression|Opioid Dependence|Methadone Treatment Centre hospitalier de l''Université de Montréal (CHUM)|Pfizer July 2014 Phase 4
NCT00888862 Unknown status Drug: Desvenlafaxine Succinate Major Depressive Disorder|Menopausal Staging and Vasomotor Symptoms (for Females) Hamilton Health Sciences Corporation|Wyeth is now a wholly owned subsidiary of Pfizer|St. Joseph''s Healthcare Hamilton|McMaster University June 2009 Phase 3
NCT00818155 Completed Drug: desvenlafaxine succinate SR|Other: Placebo Healthy Wyeth is now a wholly owned subsidiary of Pfizer January 2009 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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