Amitifadine hydrochloride
Based on 1 Customer Validation
Amitifadine (DOV-21947; EB-1010) hydrochloride is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI), with IC50s of 12, 23, 96 nM for serotonin, norepinephrine and dopamine in HEK 293 cells , respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.64%
- No. CAS: 410074-74-7
- Fòrmula: C11H12Cl3N
- Peso molecular:264.58
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Almacenamiento:
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Actividad biológica
IC50: 12 nM (serotonin), 23 nM (norepinephrine), 96 nM (dopamine)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
159 nM
Compound: DOV21947
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Inhibition of [3H]dopamine uptake at human DAT expressed in CHO cells after 10 mins by scintillation counting
Inhibition of [3H]dopamine uptake at human DAT expressed in CHO cells after 10 mins by scintillation counting
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[PMID: 22608762] |
| CHO | IC50 |
411 nM
Compound: DOV21947
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Inhibition of [3H]serotonin uptake at human SERT expressed in CHO cells after 10 min by scintillation counting
Inhibition of [3H]serotonin uptake at human SERT expressed in CHO cells after 10 min by scintillation counting
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[PMID: 22608762] |
| CHO | IC50 |
71 nM
Compound: DOV21947
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Inhibition of [3H]noradrenaline uptake at human NET expressed in CHO cells after 10 mins by scintillation counting
Inhibition of [3H]noradrenaline uptake at human NET expressed in CHO cells after 10 mins by scintillation counting
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[PMID: 22608762] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 410074-74-7
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Appearance Solid
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Peso molecular 264.58
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Fòrmula C11H12Cl3N
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Color White to off-white
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SMILES
ClC(C=C1[C@]2(CNC3)[C@@H]3C2)=C(C=C1)Cl.[H]Cl
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Synonyms
DOV-21947 hydrochloride; EB-1010 hydrochloride
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (377.96 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 50 mg/mL (188.98 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
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: ≥ 2.75 mg/mL (10.39 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: ≥ 2.75 mg/mL (10.39 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: 10 mg/mL (37.80 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.
Pureza y Documentación
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Ficha de datos (271 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Levin ED, et al. Amitifadine, a triple monoamine re-uptake inhibitor, reduces nicotine self-administration in female rats. Eur J Pharmacol. 2015 Jun 20;764:30-37. [Content Brief]
[2]. Skolnick P1, et al. Antidepressant-like actions of DOV 21,947: a "triple" reuptake inhibitor. Eur J Pharmacol. 2003 Feb 14;461(2-3):99-104. [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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 3.7796 mL | 18.8979 mL | 37.7958 mL | 94.4894 mL |
| 5 mM | 0.7559 mL | 3.7796 mL | 7.5592 mL | 18.8979 mL | |
| 10 mM | 0.3780 mL | 1.8898 mL | 3.7796 mL | 9.4489 mL | |
| 15 mM | 0.2520 mL | 1.2599 mL | 2.5197 mL | 6.2993 mL | |
| 20 mM | 0.1890 mL | 0.9449 mL | 1.8898 mL | 4.7245 mL | |
| 25 mM | 0.1512 mL | 0.7559 mL | 1.5118 mL | 3.7796 mL | |
| 30 mM | 0.1260 mL | 0.6299 mL | 1.2599 mL | 3.1496 mL | |
| 40 mM | 0.0945 mL | 0.4724 mL | 0.9449 mL | 2.3622 mL | |
| 50 mM | 0.0756 mL | 0.3780 mL | 0.7559 mL | 1.8898 mL | |
| 60 mM | 0.0630 mL | 0.3150 mL | 0.6299 mL | 1.5748 mL | |
| 80 mM | 0.0472 mL | 0.2362 mL | 0.4724 mL | 1.1811 mL | |
| 100 mM | 0.0378 mL | 0.1890 mL | 0.3780 mL | 0.9449 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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