Desvenlafaxine Succinate (WY 45233; O-Desmethylvenlafaxine)

Alias: WY 45233 Succinate; WY-45233; Pristiq; WY45233; WY 45233; Desfax

Cat No.:V1033 Purity: ≥98%

COA Product Data Instructions for use SDS

Desvenlafaxine Succinate (WY 45233; O-Desmethylvenlafaxine) Chemical Structure CAS No.: 448904-47-0
Product category: 5-HT Receptor

This product is for research use only, not for human use. We do not sell to patients.

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10mg
25mg
50mg
100mg
250mg
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1g
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Other Forms of Desvenlafaxine Succinate (WY 45233; O-Desmethylvenlafaxine):

Official Supplier of:

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

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Cancer Cell 2021,39(4):529-547.e7.

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Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

Desvenlafaxine Succinate (formerly WY45233; WY 45233; O-desmethylvenlafaxine; trade name Pristiq, Desfax), the succinate salt of Desvenlafaxine which is an approved antidepressant drug, is a novel and potent serotonin (5-HT) transporter and norepinephrine (NE) transporter reuptake inhibitor with Ki of 40.2 nM and 558.4 nM respectively. The active metabolite of the antidepressant venlafaxine, which is marketed under the trade names Effexor and Efexor, is called desvenlafaxine. Like venlafaxine, desvenlafaxine blocks serotonin and norepinephrine from being absorbed by neurons. The human dopamine (DA) transporter exhibits a weak binding affinity (62% inhibition at 100 μM) for desvenlafaxine. Desvenlafaxine is being targeted as the first non-hormonal based treatment for menopause.

Biological Activity I Assay Protocols (From Reference)

Targets

hSERT ( IC50 = 47.3 nM ); hNET ( IC50 = 531.3 nM )

ln Vitro

In vitro activity: Desvenlafaxine succinate possesses the capacity to inhibit CYP2D6, which might lead to higher concentrations of medications metabolized via this route. Additionally, desvenlafaxine succinate induces CYP3A4, which may have an effect on how medications metabolized by this enzyme are metabolized[2].

ln Vivo

Desvenlafaxine succinate (30 mg/kg, orally) increases extracellular NE levels dramatically[1], but microdialysis had no effect on DA levels.

Animal Protocol

Dissolved in 0.25% Tween 80 and 0.5% methylcellulose; 30 mg/kg; oral gavage

Male Sprague-Dawley rats

References

[1]. Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor. J Pharmacol Exp Ther. 2006 Aug;318(2):657-65.

[2]. Desvenlafaxine: another "me too" drug? Ann Pharmacother. 2008 Oct;42(10):1439-46.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C20H31NO6

Molecular Weight

381.46

Exact Mass

381.22

CAS #

448904-47-0

Related CAS #

Desvenlafaxine; 93413-62-8; Desvenlafaxine succinate hydrate; 386750-22-7; Desvenlafaxine fumarate; 93414-04-1

SMILES

CN(C)CC(C1=CC=C(C=C1)O)C2(CCCCC2)O.C(CC(=O)O)C(=O)O

InChi Key

ORUUBRMVQCKYHB-UHFFFAOYSA-N

InChi Code

InChI=1S/C16H25NO2.C4H6O4/c1-17(2)12-15(13-6-8-14(18)9-7-13)16(19)10-4-3-5-11-16;5-3(6)1-2-4(7)8/h6-9,15,18-19H,3-5,10-12H2,1-2H3;1-2H2,(H,5,6)(H,7,8)

Chemical Name

butanedioic acid;4-[2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenol

Synonyms

WY 45233 Succinate; WY-45233; Pristiq; WY45233; WY 45233; Desfax

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: ~80 mg/mL (~209.7 mM)

Water: <1 mg/mL

Ethanol: <1 mg/mL

Solubility (In Vivo)

0.5% methylcellulose+0.2%Tween 80: 30 mg/mL

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.6215 mL	13.1075 mL	26.2151 mL
	5 mM	0.5243 mL	2.6215 mL	5.2430 mL
	10 mM	0.2622 mL	1.3108 mL	2.6215 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

Calculate Reset

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculate Reset

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

Calculate Reset

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

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

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT00818155	Completed	Drug: desvenlafaxine succinate SR Other: Placebo	Healthy	Wyeth is now a wholly owned subsidiary of Pfizer	January 2009	Phase 1
NCT01948895	Completed	Drug: Desvenlafaxine	Dysthymic Disorder	Centre for Addiction and Mental Health	August 2012	Not Applicable
NCT01309542	Completed	Drug: Desvenlafaxine Succinate	Major Depressive Disorder	Pfizer	August 2003	Phase 3
NCT00887224	Completed	Drug: Placebo Drug: Desvenlafaxine succinate sustained release 50 mg	Major Depressive Disorder	Pfizer	June 2009	Phase 3
NCT00683800	Completed	Drug: Placebo Drug: desvenlafaxine succinate (DVS) SR	Vasomotor Symptoms	Pfizer	June 2008	Phase 3

Biological Data

DVS competes for the binding of radioligands specific to the serotonin (membrane) (A) and norepinephrine (whole-cell) (B) transporters, whereas weak competition was noted for the radioligand specific to the dopamine (membrane) (C) transporter.J Pharmacol Exp Ther.2006 Aug;318(2):657-65.

Desvenlafaxine Succinate — A-C, DVS increases extracellular levels of serotonin (A) and norepinephrine (B) without increasing dopamine (C) in the rat hypothalamus compared with baseline.J Pharmacol Exp Ther.2006 Aug;318(2):657-65.