Desvenlafaxine
Based on 1 Customer Validation
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.
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- 純度: 99.76%
- CAS 番号: 93413-62-8
- 分子式: C16H25NO2
- 分子量:263.38
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
IC50: 47.3 nM (hSERT), 531.3 nM (hNET)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
1500 nM
Compound: 7
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Displacement of [3H]Nisoxetine from human NET transfected in HEK293 cells after 3 hrs by Wallac counting analysis
Displacement of [3H]Nisoxetine from human NET transfected in HEK293 cells after 3 hrs by Wallac counting analysis
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[PMID: 24900709] |
| HEK293 | IC50 |
17 nM
Compound: 7
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Displacement of [3H]citalopram from human SERT transfected in HEK293 cells after 3 hrs by Wallac counting analysis
Displacement of [3H]citalopram from human SERT transfected in HEK293 cells after 3 hrs by Wallac counting analysis
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[PMID: 24900709] |
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].
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.
化学情報
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CAS 番号 93413-62-8
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性状 Solid
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分子量 263.38
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分子式 C16H25NO2
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Color White to off-white
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SMILES
OC1=CC=C(C(C2(O)CCCCC2)CN(C)C)C=C1
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別名
O-Desmethylvenlafaxine
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 50 mg/mL (189.84 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (274 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 KB)
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取扱説明書 (2659 KB)
参考文献
[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. [Content Brief]
[2]. Sopko, M.A., Jr., M.J. Ehret, and M. Grgas, Desvenlafaxine: another "me too" drug? Ann Pharmacother, 2008. 42(10): p. 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 | 3.7968 mL | 18.9840 mL | 37.9680 mL | 94.9199 mL |
| 5 mM | 0.7594 mL | 3.7968 mL | 7.5936 mL | 18.9840 mL | |
| 10 mM | 0.3797 mL | 1.8984 mL | 3.7968 mL | 9.4920 mL | |
| 15 mM | 0.2531 mL | 1.2656 mL | 2.5312 mL | 6.3280 mL | |
| 20 mM | 0.1898 mL | 0.9492 mL | 1.8984 mL | 4.7460 mL | |
| 25 mM | 0.1519 mL | 0.7594 mL | 1.5187 mL | 3.7968 mL | |
| 30 mM | 0.1266 mL | 0.6328 mL | 1.2656 mL | 3.1640 mL | |
| 40 mM | 0.0949 mL | 0.4746 mL | 0.9492 mL | 2.3730 mL | |
| 50 mM | 0.0759 mL | 0.3797 mL | 0.7594 mL | 1.8984 mL | |
| 60 mM | 0.0633 mL | 0.3164 mL | 0.6328 mL | 1.5820 mL | |
| 80 mM | 0.0475 mL | 0.2373 mL | 0.4746 mL | 1.1865 mL | |
| 100 mM | 0.0380 mL | 0.1898 mL | 0.3797 mL | 0.9492 mL |
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