DOV-216,303 Free Base
Based on 1 Customer Validation
DOV-216,303 (Free Base) is a potent triple serotonin, norepinephrine, and dopamine reuptake inhibitor, with IC50 values of 14 nM, 20 nM and 78 nM for hSERT, hNET and hDAT, respectively. Has antidepressant-like effects and increases monoamine release in the prefrontal cortex of olfactory bulbectomized (OBX) rats.
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- Pureza: 98.17%
- No. CAS: 66504-40-3
- Fòrmula: C11H11Cl2N
- Peso molecular:228.12
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Almacenamiento:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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Help & FAQs
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Actividad biológica
IC50: 14 nM (serotonin), 20 nM (norepinephrine), 78 nM (dopamine)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
143 nM
Compound: DOV216,303
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Inhibition of norepinephrine reuptake at human NET expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
Inhibition of norepinephrine reuptake at human NET expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
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[PMID: 24974340] |
| HEK293 | IC50 |
394 nM
Compound: DOV216,303
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Inhibition of DA reuptake at human DAT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
Inhibition of DA reuptake at human DAT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
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[PMID: 24974340] |
| HEK293 | IC50 |
723 nM
Compound: DOV216,303
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Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
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[PMID: 24974340] |
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Animal Model:Male Sprague Dawley rats weighing between 290 and 350 g at time of OBX or Sham surgery[2].
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Dosage:20 mg/kg.
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Administration:I.P. daily for 17days.
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Result:Increased extracellular concentrations of dopamine, norepinephrine and serotonin in the medial prefrontal cortex of both OBX and Sham animals and significantly increased extracellular baseline serotonin concentrations.
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Animal Model:Male Sprague Dawley rats weighing between 290 and 350 g at time of OBX or Sham surgery[2].
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Dosage:20 mg/kg.
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Administration:I.P. once.
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Result:Significant increases in dopamine, norepinephrine and serotonin levels were measured in both OBX and Sham animals.
Chemical Information
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No. CAS 66504-40-3
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Appearance Oil
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Peso molecular 228.12
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Fòrmula C11H11Cl2N
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Color Colorless to light yellow
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SMILES
ClC1=C(Cl)C=C(C=C1)C12CC1CNC2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : ≥ 125 mg/mL (547.96 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 100 mg/mL (438.37 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. 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)
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: ≥ 2.08 mg/mL (9.12 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
Pureza y Documentación
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Ficha de datos (276 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
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 |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 4.3837 mL | 21.9183 mL | 43.8366 mL | 109.5914 mL |
| 5 mM | 0.8767 mL | 4.3837 mL | 8.7673 mL | 21.9183 mL | |
| 10 mM | 0.4384 mL | 2.1918 mL | 4.3837 mL | 10.9591 mL | |
| 15 mM | 0.2922 mL | 1.4612 mL | 2.9224 mL | 7.3061 mL | |
| 20 mM | 0.2192 mL | 1.0959 mL | 2.1918 mL | 5.4796 mL | |
| 25 mM | 0.1753 mL | 0.8767 mL | 1.7535 mL | 4.3837 mL | |
| 30 mM | 0.1461 mL | 0.7306 mL | 1.4612 mL | 3.6530 mL | |
| 40 mM | 0.1096 mL | 0.5480 mL | 1.0959 mL | 2.7398 mL | |
| 50 mM | 0.0877 mL | 0.4384 mL | 0.8767 mL | 2.1918 mL | |
| 60 mM | 0.0731 mL | 0.3653 mL | 0.7306 mL | 1.8265 mL | |
| 80 mM | 0.0548 mL | 0.2740 mL | 0.5480 mL | 1.3699 mL | |
| 100 mM | 0.0438 mL | 0.2192 mL | 0.4384 mL | 1.0959 mL |
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