Azatadine dimaleate
Based on 1 Customer Validation
Azatadine dimaleate (Azatadine maleate) is an orally active histamine H1 receptor inhibitor, cetylcholine receptor inhibitor, and serotonin receptor inhibitor. Azatadine dimaleate induces sedation and exhibits topical anesthetic properties. Azatadine dimaleate can be used for the research of allergic rhinitis.
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- Pureza: 99.85%
- No. CAS: 3978-86-7
- Fòrmula: C28H30N2O8
- Peso molecular:522.55
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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
Azatadine dimaleate (3.4 nM-13 nM; 3 minutes) competitively inhibits Histamine (HY-B1204)-induced contractions in isolated guinea-pig ileum segments with an ED50 of 6.5 nM[1].
Azatadine dimaleate (6.8 nM-27 nM; 3 minutes) competitively inhibits acetylcholine-induced contractions in isolated guinea-pig ileum segments with an ED50 of 10 nM[1].
Azatadine dimaleate (6.8 nM-27 nM; 3 minutes) inhibits Serotonin (HY-B1473A)-induced contractions in isolated unprimed virgin rat uterus segments with an ED50 of 14 nM[1].
Azatadine dimaleate (50 μM-1 mM) dose-dependently inhibits anti-IgE-induced Histamine and Leukotriene C4 (HY-113446) release from human lung mast cells, with significantly greater inhibition of Leukotriene C4 release (85% at 1 mM) compared to histamine release (45% at 1 mM)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Azatadine dimaleate (p.o.; single dose) potently delays the onset of Histamine-induced dyspnea in guinea-pigs, with an oral ED200 of 0.01 mg/kg[1].
Azatadine dimaleate (p.o.; single dose) delays the onset of acetylcholine-induced dyspnea in guinea-pigs, with an oral ED200 of 0.739 mg/kg[1].
Azatadine dimaleate (p.o.; single dose) delays the onset of Serotonin-induced dyspnea in guinea-pigs with an oral ED200 of 0.860 mg/kg[1].
Azatadine dimaleate (p.o.; single dose) exhibits potent antianaphylactic activity in sensitized guinea-pigs, with an oral PD50 of 0.024 mg/kg for protection against anaphylactic shock[1].
Azatadine dimaleate (p.o.; single dose) potently protects pertussis-sensitized mice against Histamine-induced lethality, with an oral PD50 of 0.022 mg/kg[1].
Azatadine dimaleate (p.o.; single dose) exhibits potent antianaphylactic activity in sensitized mice, with an oral PD50 of 0.019 mg/kg for protection against anaphylactic shock[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 3978-86-7
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Appearance Solid
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Peso molecular 522.55
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Fòrmula C28H30N2O8
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Color White to off-white
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SMILES
O=C(O)/C=C\C(O)=O.O=C(O)/C=C\C(O)=O.CN1CC/C(CC1)=C2C3=CC=CC=C3CCC4=CC=CN=C4\2
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Synonyms
Azatadine maleate
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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
H2O : ≥ 100 mg/mL (191.37 mM)
DMSO : ≥ 100 mg/mL (191.37 mM; 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). 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: ≥ 2.5 mg/mL (4.78 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 (4.78 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: 100 mg/mL (191.37 mM); Clear solution; Need ultrasonic
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 (281 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Tozzi S, et al. The pharmacology of azatadine, a potential antiallergy drug. Agents Actions. 1974 Oct;4(4):264-70. [Content Brief]
[2]. Katelaris C, et al. Comparative effects of loratadine and azatadine in the treatment of seasonal allergic rhinitis. Asian Pac J Allergy Immunol. 1990;8(2):103-107. [Content Brief]
[3]. Togias AG, et al. Demonstration of inhibition of mediator release from human mast cells by azatadine base. In vivo and in vitro evaluation. JAMA. 1986 Jan 10;255(2):225-9. [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 | 1.9137 mL | 9.5685 mL | 19.1369 mL | 47.8423 mL |
| 5 mM | 0.3827 mL | 1.9137 mL | 3.8274 mL | 9.5685 mL | |
| 10 mM | 0.1914 mL | 0.9568 mL | 1.9137 mL | 4.7842 mL | |
| 15 mM | 0.1276 mL | 0.6379 mL | 1.2758 mL | 3.1895 mL | |
| 20 mM | 0.0957 mL | 0.4784 mL | 0.9568 mL | 2.3921 mL | |
| 25 mM | 0.0765 mL | 0.3827 mL | 0.7655 mL | 1.9137 mL | |
| 30 mM | 0.0638 mL | 0.3189 mL | 0.6379 mL | 1.5947 mL | |
| 40 mM | 0.0478 mL | 0.2392 mL | 0.4784 mL | 1.1961 mL | |
| 50 mM | 0.0383 mL | 0.1914 mL | 0.3827 mL | 0.9568 mL | |
| 60 mM | 0.0319 mL | 0.1595 mL | 0.3189 mL | 0.7974 mL | |
| 80 mM | 0.0239 mL | 0.1196 mL | 0.2392 mL | 0.5980 mL | |
| 100 mM | 0.0191 mL | 0.0957 mL | 0.1914 mL | 0.4784 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.
Azatadine dimaleate Related Classifications
HY-B0170A Related Classifications
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