Catalog No.S4113 Synonyms: WY 45233 Succinate
Molecular Weight(MW): 263.38
Desvenlafaxine is a serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor with Ki of 40.2 nM and 558.4 nM, respectively.
Purity & Quality Control
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|Description||Desvenlafaxine is a serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor with Ki of 40.2 nM and 558.4 nM, respectively.|
|Features||Desvenlafaxine is a major active metabolite of venlafaxine.|
Desvenlafaxine is a serotonin-norepinephrine reuptake inhibitor and is the active metabolite of the antidepressant venlafaxine. Similar to venlafaxine, desvenlafaxine inhibits the neuronal uptake of serotonin and norepinephrine. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter. Desvenlafaxine inhibits [3H]5-HT or [3H]NE uptake for the hSERT or hNET with IC50 of 47.3 and 531.3 nM, respectively. Desvenlafaxine 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, which could impact the metabolism of drugs metabolized via this enzyme. 
|In vivo||Desvenlafaxine rapidly penetrates the male rat brain and hypothalamus. Desvenlafaxine significantly increases extracellular NE levels compared with baseline in the male rat hypothalamus but had no effect on DA levels using microdialysis.  Desvenlafaxine 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%.|
|In vitro||DMSO||37 mg/mL (140.48 mM)|
|Ethanol||3 mg/mL (11.39 mM)|
|In vivo||Add solvents individually and in order:
0.5% methylcellulose+0.2% Tween 80
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||WY 45233 Succinate|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02859103||Not yet recruiting||Depression|Anhedonia||St. Michaels Hospital, Toronto||November 2016||Phase 4|
|NCT02819921||Not yet recruiting||Hot Flashes|Breast Neoplasms||Seoul National University Hospital|Seoul National University Bundang Hospital|Korea Cancer Center Hospital|Pfizer||September 2016||Phase 4|
|NCT02330679||Unknown status||Major Depressive Disorder||University of Calgary|University of Alberta||December 2014||Phase 4|
|NCT02200406||Recruiting||Depression|Opioid Dependence|Methadone Treatment||Didier Jutras-Aswad|Pfizer|Centre hospitalier de lUniversité de Montréal (CHUM)||July 2014||Phase 4|
|NCT01974934||Recruiting||Vascular Depression||Hotel-Dieu Grace Healthcare||December 2013||Phase 4|
|NCT01977378||Unknown status||Major Depressive Disorder||Jiangsu Hansoh Pharmaceutical Co., Ltd.||October 2013||Phase 2|Phase 3|
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.
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