Tiapride hydrochloride
Based on 1 Customer Validation
Tiapride hydrochloride is a selective and orally active D2 and D3 dopamine receptors antagonist with IC50 values of 110-320 nM and 180 nM, respectively. Tiapride hydrochloride shows anti-dyskinetic activity and anxiolytic activity. Tiapride hydrochloride is a neuroleptic agent.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.95%
- CAS. Nr.: 51012-33-0
- Formel: C15H25ClN2O4S
- Molecular Weight:364.89
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Speicherung:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
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D2 Receptor 110-320 nM (IC50) |
D3 Receptor 180 nM (IC50) |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mouse ethanol-induced hyperactivity models[2]
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Dosage:10-200 mg/kg
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Administration:ip
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Result:Inhibited the hyperactivity.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 51012-33-0
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Appearance Solid
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Molecular Weight 364.89
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Formel C15H25ClN2O4S
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Color White to off-white
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SMILES
O=C(NCCN(CC)CC)C1=CC(S(=O)(C)=O)=CC=C1OC.[H]Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Lösungsmittel & Löslichkeit
In Vitro:
H2O : ≥ 200 mg/mL (548.11 mM)
DMSO : 31.25 mg/mL (85.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" 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 and light). 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 and light). 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
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: ≥ 0.62 mg/mL (1.70 mM); Clear solution
This protocol yields a clear solution of ≥ 0.62 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.2 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: ≥ 0.62 mg/mL (1.70 mM); Clear solution
This protocol yields a clear solution of ≥ 0.62 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.2 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: 100 mg/mL (274.06 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
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.
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Protocol for Elevated Plus Maze Test
The Elevated Plus Maze is a rodent anxiety-like behavior assay based on the conflict between spontaneous exploration and avoidance of open, elevated, exposed spaces. The apparatus contains two open arms and two closed arms arranged in a plus shape, and rodents normally spend more time in closed arms than open arms. The assay readout is generated by recording arm entries, time spent in open and closed arms, and related exploratory behaviors. Increased open-arm time or open-arm entries is commonly interpreted as reduced anxiety-like behavior, whereas reduced open-arm exploration is interpreted as increased anxiety-like behavior.
Reinheit & Dokumentation
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Data Sheet (273 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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Scatton B, et al. The preclinical pharmacologic profile of tiapride. Eur Psychiatry. 2001 Jan;16 Suppl 1:29s-34s. [Content Brief]
[2]. Peters DH, et al. Tiapride. A review of its pharmacology and therapeutic potential in the management of alcohol dependence syndrome. Drugs. 1994 Jun;47(6):1010-32. [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 and light). 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 | 2.7406 mL | 13.7028 mL | 27.4055 mL | 68.5138 mL |
| 5 mM | 0.5481 mL | 2.7406 mL | 5.4811 mL | 13.7028 mL | |
| 10 mM | 0.2741 mL | 1.3703 mL | 2.7406 mL | 6.8514 mL | |
| 15 mM | 0.1827 mL | 0.9135 mL | 1.8270 mL | 4.5676 mL | |
| 20 mM | 0.1370 mL | 0.6851 mL | 1.3703 mL | 3.4257 mL | |
| 25 mM | 0.1096 mL | 0.5481 mL | 1.0962 mL | 2.7406 mL | |
| 30 mM | 0.0914 mL | 0.4568 mL | 0.9135 mL | 2.2838 mL | |
| 40 mM | 0.0685 mL | 0.3426 mL | 0.6851 mL | 1.7128 mL | |
| 50 mM | 0.0548 mL | 0.2741 mL | 0.5481 mL | 1.3703 mL | |
| 60 mM | 0.0457 mL | 0.2284 mL | 0.4568 mL | 1.1419 mL | |
| 80 mM | 0.0343 mL | 0.1713 mL | 0.3426 mL | 0.8564 mL | |
| H2O | 100 mM | 0.0274 mL | 0.1370 mL | 0.2741 mL | 0.6851 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.
Tiapride hydrochloride Related Classifications
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