Desvenlafaxine

Catalog No.S4113 Batch:S411301

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Technical Data

Formula

C16H25NO2

Molecular Weight 263.38 CAS No. 93413-62-8
Solubility (25°C)* In vitro DMSO 37 mg/mL (140.48 mM)
Ethanol 3 mg/mL (11.39 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
0.5% methylcellulose 0.2% Tween 80
10.0mg/ml 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. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Desvenlafaxine (WY 45233 Succinate) is a serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor with Ki of 40.2 nM and 558.4 nM, respectively.
Targets
5-HT [1] Norepinephrine (NE) [1]
40.2 nM(Ki) 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, 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.[1] 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. [2]
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. [1] 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%.[2]
Features Desvenlafaxine is a major active metabolite of venlafaxine.

Protocol (from reference)

Animal Study:[1]
  • Animal Models

    Male Sprague-Dawley rats

  • Dosages

    30 mg/kg

  • Administration

    oral

Selleck's Desvenlafaxine has been cited by 2 publications

Duloxetine enhances the sensitivity of non-small cell lung cancer cells to EGFR inhibitors by REDD1-induced mTORC1/S6K1 suppression [ Am J Cancer Res, 2024, 14(3):1087-1100] PubMed: 38590408
Influence of Zuojin Pill on the Metabolism of Venlafaxine in Vitro and in Rats and Associated Herb-Drug Interaction [ Drug Metab Dispos, 2020, 48(10):1044-1052] PubMed: 32561594

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.