Rizatriptan benzoate
Based on 1 Customer Validation
Rizatriptan benzoate is the agonist for 5-HT1B and 5-HT1D. Rizatriptan benzoate has a peripheral vasoconstrictive effect, penetrates the intact blood-brain barrier, and inhibits pain neurotransmission in the central nervous system.
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- Pureté : 99.93%
- CAS No.: 145202-66-0
- Formule: C22H25N5O2
- Masse moléculaire:391.47
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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
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Activité biologique
Description
IC50 & Target
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5-HT1B Receptor |
5-HT1D Receptor |
5-HT1 Receptor |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Dural stimulation in the trigeminal nucleus caudalis of rats models[2]
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Dosage:0.3-3 mg/kg
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Administration:iv, every 10 min for 1 h
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Result:Inhibited the pain response.
Chemical Information
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CAS No. 145202-66-0
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Appearance Solid
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Masse moléculaire 391.47
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Formule C22H25N5O2
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Color White to off-white
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SMILES
CN(C)CCC1=CNC2=C1C=C(CN3N=CN=C3)C=C2.O=C(O)C4=CC=CC=C4
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Synonyms
MK 462
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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:
H2O : 100 mg/mL (255.45 mM; Need ultrasonic)
DMSO : 50 mg/mL (127.72 mM; Need ultrasonic; 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.
* 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)
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: ≥ 2.5 mg/mL (6.39 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 (6.39 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: 50 mg/mL (127.72 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.
Pureté et documentation
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Fiche technique (272 KB)
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SDS (418 KB)
- English - EN (418 KB)
- Français - FR (418 KB)
- Deutsch - DE (418 KB)
- Norwegian - NO (418 KB)
- Español - ES (418 KB)
- Swedish - SV (418 KB)
- Italian - IT (418 KB)
- Korean - KR (418 KB)
- Portuguese - PT (418 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Sciberras DG, et al. Initial human experience with MK-462 (rizatriptan): a novel 5-HT1D agonist. Br J Clin Pharmacol. 1997 Jan;43(1):49-54. [Content Brief]
[2]. Cumberbatch MJ, et al. Rizatriptan has central antinociceptive effects against durally evoked responses. Eur J Pharmacol. 1997 Jun 5;328(1):37-40. [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 |
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| DMSO / H2O | 1 mM | 2.5545 mL | 12.7724 mL | 25.5447 mL | 63.8619 mL |
| 5 mM | 0.5109 mL | 2.5545 mL | 5.1089 mL | 12.7724 mL | |
| 10 mM | 0.2554 mL | 1.2772 mL | 2.5545 mL | 6.3862 mL | |
| 15 mM | 0.1703 mL | 0.8515 mL | 1.7030 mL | 4.2575 mL | |
| 20 mM | 0.1277 mL | 0.6386 mL | 1.2772 mL | 3.1931 mL | |
| 25 mM | 0.1022 mL | 0.5109 mL | 1.0218 mL | 2.5545 mL | |
| 30 mM | 0.0851 mL | 0.4257 mL | 0.8515 mL | 2.1287 mL | |
| 40 mM | 0.0639 mL | 0.3193 mL | 0.6386 mL | 1.5965 mL | |
| 50 mM | 0.0511 mL | 0.2554 mL | 0.5109 mL | 1.2772 mL | |
| 60 mM | 0.0426 mL | 0.2129 mL | 0.4257 mL | 1.0644 mL | |
| 80 mM | 0.0319 mL | 0.1597 mL | 0.3193 mL | 0.7983 mL | |
| 100 mM | 0.0255 mL | 0.1277 mL | 0.2554 mL | 0.6386 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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