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Desvenlafaxine (Synonyms: Desvenlafaxine, DVS 233, MDD-XR)

Catalog No.GC11570

serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor

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Desvenlafaxine Chemical Structure

Cas No.: 93413-62-8

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10mM (in 1mL DMSO)
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25mg
$14.00
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100mg
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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Product Documents

Quality Control & SDS

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Background

Desvenlafaxine is a serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor with Ki of 40.2 nM and 558.4 nM, respectively. Target: SSRIsDesvenlafaxine 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. 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 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. 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].

References:
[1]. Deecher, D.C., et al., Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor. J Pharmacol Exp Ther, 2006. 318(2): p. 657-65.
[2]. Sopko, M.A., Jr., M.J. Ehret, and M. Grgas, Desvenlafaxine: another "me too" drug Ann Pharmacother, 2008. 42(10): p. 1439-46.

Chemical Properties

Cas No. 93413-62-8 SDF
Synonyms Desvenlafaxine, DVS 233, MDD-XR
Chemical Name 4-[2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenol
Canonical SMILES CN(C)CC(C1=CC=C(C=C1)O)C2(CCCCC2)O
Formula C16H25NO2 M.Wt 263.38
Solubility ≥ 13.2mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 3.7968 mL 18.984 mL 37.968 mL
5 mM 0.7594 mL 3.7968 mL 7.5936 mL
10 mM 0.3797 mL 1.8984 mL 3.7968 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 12 reference(s) in Google Scholar.)

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