1. Neuronal Signaling
  2. Serotonin Transporter
  3. Desvenlafaxine

Desvenlafaxine (Synonyms: O-Desmethylvenlafaxine)

Cat. No.: HY-B0602 Purity: >98.0%
Handling Instructions

Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter.

For research use only. We do not sell to patients.

Desvenlafaxine Chemical Structure

Desvenlafaxine Chemical Structure

CAS No. : 93413-62-8

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Description

Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter[1][2].

IC50 & Target

IC50: 47.3 nM (hSERT), 531.3 nM (hNET)[1].

In Vitro

Desvenlafaxine has the potential to inhibit CYP2D6, which could result in increased concentrations of drugs metabolized through this pathway. Desvenlafaxine also induces CYP3A4, which could impact the metabolism of drugs metabolized via this enzyme[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male rats[1].
Dosage: 30 mg/kg.
Administration: Orally.
Result: Significantly increased extracellular NE levels compared with baseline in the male rat hypothalamus but had no effect on DA levels using microdialysis.
Clinical Trial
Molecular Weight

263.38

Formula

C₁₆H₂₅NO₂

CAS No.

93413-62-8

SMILES

OC1=CC=C(C(C2(O)CCCCC2)CN(C)C)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (189.84 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7968 mL 18.9840 mL 37.9680 mL
5 mM 0.7594 mL 3.7968 mL 7.5936 mL
10 mM 0.3797 mL 1.8984 mL 3.7968 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (9.49 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (9.49 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.49 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: >98.0%

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Keywords:

DesvenlafaxineO-DesmethylvenlafaxineSerotonin Transporter5-HTTSERTSLC6A4Inhibitorinhibitorinhibit

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Desvenlafaxine
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