Tasipimidine sulfate
Based on 1 Customer Validation
Tasipimidine sulfate is an orally active and selective α2A-adrenoceptor agonist with a pEC50 of 7.57 for human α2A-adrenoceptors and an EC50 of 5.7 nM for rat α2-adrenoceptor. Tasipimidine sulfate can be utilized in research related to situational anxiety and fear.
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- Pureté : 99.32%
- CAS No.: 1465908-73-9
- Formule: C13H18N2O6S
- Masse moléculaire:330.36
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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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
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Activité biologique
Description
IC50 & Target
[1]|
human α2A-adrenoceptor 7.57 (pEC50) |
rat α2-adrenergic receptor 5.7 nM (EC50) |
In Vivo
Tasipimidine (300-1000 μg/kg; subcutaneous injection; single dose) sulfate reduces the amplitude of the acoustic startle reflex in rats, with onset within 20 minutes, peak effect at 1 hour, and duration of at least 2 hours[1].
Tasipimidine (10-30 μg/kg; oral administration; total 3 treatment cycles) sulfate has an improving effect on separation anxiety in dogs[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Non-habituated mice[1]
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Dosage:Subcutaneous injection: 10, 30 and 100 μg/kg
Oral administration: 900 and 3000 μg/kg -
Administration:Single dose
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Result:Significantly reduced the activity count at doses of 30 μg/kg and higher doses, with 100 μg/kg showing a more pronounced effect by subcutaneous injection.
Significantly decreased the spontaneous locomotor activity of 3.0 mg/kg, while 0.9 mg/kg had no effect by oral administration.
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Animal Model:Clinically healthy privately-owned dogs with a history of separation anxiety[2]
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Dosage:10 and 30 μg/kg
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Administration:Oral administration; three 4-day treatment periods in randomized order each followed by a 3-day washout
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Result:Had a statistically significant treatment effect.
Led to more positive owner ratings, significantly reduced destructive/rearranging behavior and vocalization at dose of 30 μg/kg. Most dogs remained fully responsive and able to walk normally, with no serious adverse events reported.
Chemical Information
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CAS No. 1465908-73-9
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Appearance Solid
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Masse moléculaire 330.36
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Formule C13H18N2O6S
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Color White to off-white
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SMILES
O=S(O)(O)=O.COC1=CC=CC2=C1CCOC2C3=NCCN3
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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)
Solvant et solubilité
In Vitro:
DMSO : 125 mg/mL (378.38 mM; ultrasonic and warming and heat to 60°C; 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 (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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.08 mg/mL (6.30 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.30 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 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.
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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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 |
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| DMSO | 1 mM | 3.0270 mL | 15.1350 mL | 30.2700 mL | 75.6750 mL |
| 5 mM | 0.6054 mL | 3.0270 mL | 6.0540 mL | 15.1350 mL | |
| 10 mM | 0.3027 mL | 1.5135 mL | 3.0270 mL | 7.5675 mL | |
| 15 mM | 0.2018 mL | 1.0090 mL | 2.0180 mL | 5.0450 mL | |
| 20 mM | 0.1514 mL | 0.7568 mL | 1.5135 mL | 3.7838 mL | |
| 25 mM | 0.1211 mL | 0.6054 mL | 1.2108 mL | 3.0270 mL | |
| 30 mM | 0.1009 mL | 0.5045 mL | 1.0090 mL | 2.5225 mL | |
| 40 mM | 0.0757 mL | 0.3784 mL | 0.7568 mL | 1.8919 mL | |
| 50 mM | 0.0605 mL | 0.3027 mL | 0.6054 mL | 1.5135 mL | |
| 60 mM | 0.0505 mL | 0.2523 mL | 0.5045 mL | 1.2613 mL | |
| 80 mM | 0.0378 mL | 0.1892 mL | 0.3784 mL | 0.9459 mL | |
| 100 mM | 0.0303 mL | 0.1514 mL | 0.3027 mL | 0.7568 mL |
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