Name: Desvenlafaxine
Brand: Selleck Chemicals
SKU: S4113
Availability: InStock
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Quality Control

Batch: S411301 DMSO]37 mg/mL]false]Ethanol]3 mg/mL]false]Water]Insoluble]false Purity: 99.72%

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COA
NMR
HPLC
SDS
Datasheet

99.72

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE)
Other Serotonin Transporter Inhibitors	Dapoxetine

Solubility

In vitro
Batch:

DMSO : 37 mg/mL (140.48 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	0.5% methylcellulose 1 0.2% Tween 80 Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (37.97mM)	Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 0.5% methylcellulose+0.2% Tween 80 clear solution, and mix evenly to make it a uniform suspension. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

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% ddH₂O

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Calculation results:

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.

Chemical Information, Storage & Stability

Molecular Weight	263.38	Formula	C₁₆H₂₅NO₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	93413-62-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	WY 45233 Succinate			Smiles	CN(C)CC(C1=CC=C(C=C1)O)C2(CCCCC2)O

Mechanism of Action

Features	Desvenlafaxine is a major active metabolite of venlafaxine.
Targets/IC₅₀/Ki	5-HT 40.2 nM(Ki) Norepinephrine (NE) 558.4 nM(Ki)
In vitro	Desvenlafaxine is a serotonin-norepinephrine reuptake inhibitor and is the active metabolite of the antidepressant venlafaxine. Similar to venlafaxine, this compound inhibits the neuronal uptake of serotonin and norepinephrine. It shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter. This chemical inhibits [³H]5-HT or [³H]NE uptake for the hSERT or hNET with IC50 of 47.3 and 531.3 nM, respectively. It 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 this agent, which could impact the metabolism of drugs metabolized via this enzyme.
In vivo	Desvenlafaxine rapidly penetrates the male rat brain and hypothalamus. This compound significantly increases extracellular NE levels compared with baseline in the male rat hypothalamus but had no effect on DA levels using microdialysis. It 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%.
References	[1] https://pubmed.ncbi.nlm.nih.gov/16675639/ [2] https://pubmed.ncbi.nlm.nih.gov/18698015/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02637193	Completed	Healthy Subjects	Pfizer''s Upjohn has merged with Mylan to form Viatris Inc.\|Pfizer	December 2015	Phase 1
NCT02200406	Completed	Depression\|Opioid Dependence\|Methadone Treatment	Centre hospitalier de l''Université de Montréal (CHUM)\|Pfizer	July 2014	Phase 4
NCT00888862	Unknown status	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	Healthy	Wyeth is now a wholly owned subsidiary of Pfizer	January 2009	Phase 1

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Desvenlafaxine Serotonin Transporter inhibitor

Chemical Structure

Molecular Weight: 263.38