Desvenlafaxine succinate
Based on 1 Customer Validation
Desvenlafaxine succinate, 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 (DVS) shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter.
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- Purity: 98.68%
- CAS No.: 448904-47-0
- 화학식: C20H31NO6
- 분자량:381.46
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
IC50: 47.3 nM (hSERT), 531.3 nM (hNET)[1].
Desvenlafaxine succinate has the potential to inhibit CYP2D6, which could result in increased concentrations of drugs metabolized through this pathway. Desvenlafaxine succinate also induces CYP3A4, which could impact the metabolism of drugs metabolized via this enzyme[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male rats[1].
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Dosage:30 mg/kg.
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Administration:Orally.
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Result:Significantly increased extracellular NE levels compared with baseline in the male rat hypothalamus but had no effect on DA levels using microdialysis.
Chemical Information
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CAS No. 448904-47-0
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Appearance Solid
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분자량 381.46
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화학식 C20H31NO6
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SMILES
O=C(O)CCC(O)=O.OC1=CC=C(C(C2(O)CCCCC2)CN(C)C)C=C1
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Synonyms
O-Desmethylvenlafaxine succinate; Wy-45233 succinate
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (262.15 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
References
[1]. Darlene C Deecher, et al. Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor. J Pharmacol Exp Ther. 2006 Aug;318(2):657-65. [Content Brief]
[2]. Michael A Sopko Jr, et al. Desvenlafaxine: another "me too" drug? Ann Pharmacother. 2008 Oct;42(10):1439-46. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6215 mL | 13.1075 mL | 26.2151 mL | 65.5377 mL |
| 5 mM | 0.5243 mL | 2.6215 mL | 5.2430 mL | 13.1075 mL | |
| 10 mM | 0.2622 mL | 1.3108 mL | 2.6215 mL | 6.5538 mL | |
| 15 mM | 0.1748 mL | 0.8738 mL | 1.7477 mL | 4.3692 mL | |
| 20 mM | 0.1311 mL | 0.6554 mL | 1.3108 mL | 3.2769 mL | |
| 25 mM | 0.1049 mL | 0.5243 mL | 1.0486 mL | 2.6215 mL | |
| 30 mM | 0.0874 mL | 0.4369 mL | 0.8738 mL | 2.1846 mL | |
| 40 mM | 0.0655 mL | 0.3277 mL | 0.6554 mL | 1.6384 mL | |
| 50 mM | 0.0524 mL | 0.2622 mL | 0.5243 mL | 1.3108 mL | |
| 60 mM | 0.0437 mL | 0.2185 mL | 0.4369 mL | 1.0923 mL | |
| 80 mM | 0.0328 mL | 0.1638 mL | 0.3277 mL | 0.8192 mL | |
| 100 mM | 0.0262 mL | 0.1311 mL | 0.2622 mL | 0.6554 mL |