Radafaxine hydrochloride
Based on 1 publication(s) in Google Scholar
Radafaxine hydrochloride (GW-353162A) is a DAT (dopamine transporter) and NET(norepinephrine transporter) transporters inhibitor, and nAChR family modulator.
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- Pureté: 98.92%
- CAS No.: 106083-71-0
- Formule: C13H19Cl2NO2
- Masse moléculaire:292.20
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Radafaxine hydrochloride
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Activité biologique
The relatively low potency of Radafaxine hydrochloride (GW-353162A) in blocking DAT and its slow blockade suggests that it is unlikely to have reinforcing effects[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 106083-71-0
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Appearance Solid
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Masse moléculaire 292.20
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Formule C13H19Cl2NO2
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Color White to off-white
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SMILES
O[C@]1(C2=CC=CC(Cl)=C2)[C@H](C)NC(C)(C)CO1.[H]Cl
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Synonyms
(S,S)-Hydroxybupropion hydrochloride; GW-353162A; BW-306U
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Nature
2024 Sep;633(8029):473-479. PMID: 39143211
Solvant et solubilité
DMSO : 25 mg/mL (85.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 25 mg/mL (85.56 mM; Need ultrasonic)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (8.56 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 (8.56 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 8.33 mg/mL (28.51 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureté et documentation
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Fiche technique (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Xu H, et al. Stereoselective analysis of hydroxybupropion and application to drug interaction studies. Chirality. 2007 Mar;19(3):163-70. [Content Brief]
[2]. Volkow ND, et al. The slow and long-lasting blockade of dopamine transporters in human brain induced by the new antidepressant drug radafaxine predict poor reinforcing effects. Biol Psychiatry. 2005 Mar 15;57(6):640-6. [Content Brief]
[3]. Bondarev ML, et al. Behavioral and biochemical investigations of bupropion metabolites. Eur J Pharmacol. 2003 Aug 1;474(1):85-93. [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 (sealed storage, away from moisture). 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 / H2O | 1 mM | 3.4223 mL | 17.1116 mL | 34.2231 mL | 85.5578 mL |
| 5 mM | 0.6845 mL | 3.4223 mL | 6.8446 mL | 17.1116 mL | |
| 10 mM | 0.3422 mL | 1.7112 mL | 3.4223 mL | 8.5558 mL | |
| 15 mM | 0.2282 mL | 1.1408 mL | 2.2815 mL | 5.7039 mL | |
| 20 mM | 0.1711 mL | 0.8556 mL | 1.7112 mL | 4.2779 mL | |
| 25 mM | 0.1369 mL | 0.6845 mL | 1.3689 mL | 3.4223 mL | |
| 30 mM | 0.1141 mL | 0.5704 mL | 1.1408 mL | 2.8519 mL | |
| 40 mM | 0.0856 mL | 0.4278 mL | 0.8556 mL | 2.1389 mL | |
| 50 mM | 0.0684 mL | 0.3422 mL | 0.6845 mL | 1.7112 mL | |
| 60 mM | 0.0570 mL | 0.2852 mL | 0.5704 mL | 1.4260 mL | |
| 80 mM | 0.0428 mL | 0.2139 mL | 0.4278 mL | 1.0695 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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