1. Neuronal Signaling
  2. Serotonin Transporter
  3. Desvenlafaxine succinate hydrate

Desvenlafaxine succinate hydrate (Synonyms: O-Desmethylvenlafaxine succinate hydrate)

Cat. No.: HY-B0602A Purity: 99.76%
Handling Instructions

Desvenlafaxine succinate hydrate, 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 succinate hydrate shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter.

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Desvenlafaxine succinate hydrate Chemical Structure

Desvenlafaxine succinate hydrate Chemical Structure

CAS No. : 386750-22-7

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

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

In Vivo

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

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

399.48

Formula

C₂₀H₃₃NO₇

CAS No.

386750-22-7

SMILES

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

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 : ≥ 33 mg/mL (82.61 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5033 mL 12.5163 mL 25.0325 mL
5 mM 0.5007 mL 2.5033 mL 5.0065 mL
10 mM 0.2503 mL 1.2516 mL 2.5033 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: ≥ 2.08 mg/mL (5.21 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (5.21 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (5.21 mM); Clear solution

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

Purity: 99.76%

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Keywords:

Desvenlafaxine succinateO-Desmethylvenlafaxine succinateSerotonin Transporter5-HTTSERTSLC6A4Inhibitorinhibitorinhibit

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Desvenlafaxine succinate hydrate
Cat. No.:
HY-B0602A
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