Tazanolast
Based on 1 Customer Validation
Tazanolast (TO 188) is an orally active selective mast cell stabilizer. Tazanolast prevents the elevation of intracellular calcium concentration, inhibits calcium uptake and Protein kinase C translocation, without directly inhibiting phospholipase C. Tazanolast inhibits ozone-induced airway hyperresponsiveness to Methacholine in guinea pigs, as well as passive cutaneous anaphylaxis, Schultz-Dale reaction, experimental asthma, passive cutaneous anaphylaxis in rats, and increased cutaneous vascular permeability in rats. Tazanolast does not alter airway responsiveness in sham-exposed guinea pigs, cell distribution in bronchoalveolar lavage fluid after ozone exposure, type II-IV allergic reactions, or histamine release from atopic leukocytes. Tazanolast can be used in research related to allergic diseases.
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- Pureza: 99.50%
- No. CAS: 82989-25-1
- Fòrmula: C13H15N5O3
- Peso molecular:289.29
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Almacenamiento:Powder -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
Descripciòn
In Vitro
Tazanolast acts as a selective mast cell stabilizer by inhibiting multiple mast cell activation pathways, including histamine release, calcium uptake, protein kinase C translocation, and inositol trisphosphate production, and suppresses the Schultz-Dale reaction in isolated tracheal muscle[1].
Tazanolast prevents histamine release-inducing intracellular calcium concentration increases in mast cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Tazanolast (300 mg/kg; p.o.; 30 minutes before sham air exposure) does not affect baseline airway responsiveness or BAL cell distribution in healthy guinea pigs exposed to filtered air[1].
Tazanolast (10 mg/kg; p.o.) significantly inhibits Ovalbumin (HY-W250978)-induced passive cutaneous anaphylaxis in rats and potently suppresses Substance P- and PGD2-mediated increases in vascular permeability in rat skin[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Hartley (male, 400 to 600 g, ozone-induced airway hyperresponsiveness)[1]
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Dosage:30 mg/kg (pre-ozone exposure); 100 mg/kg (pre-ozone exposure); 300 mg/kg (pre-ozone exposure); 300 mg/kg (post-ozone exposure)
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Administration:p.o.; 30 minutes before ozone exposure; p.o.; immediately after ozone exposure
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Result:Inhibited ozone-induced increases in airway responsiveness in a dose-dependent manner, with delta logPC200-MCh values of 0.45 for 30 mg/kg, 0.21 for 100 mg/kg, and 0.09 for 300 mg/kg, all significantly lower than the vehicle group value of 0.65 (p < 0.05, p < 0.01, and p < 0.001, respectively).
Did not produce a delta logPC200-MCh value significantly different from the vehicle group when administered at 300 mg/kg after ozone exposure.
Did not significantly alter BAL cell distribution (neutrophils, macrophages, lymphocytes, eosinophils) at 2 hours after ozone exposure at all tested doses compared to the vehicle group.
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Animal Model:Hartley (male, 400 to 600 g, healthy, sham filtered air exposure)[1]
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Dosage:300 mg/kg
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Administration:p.o.; 30 minutes before sham air exposure
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Result:Did not alter PC200-MCh compared to baseline values or the vehicle-treated sham exposure group.
Showed no significant differences in BAL cell numbers (macrophages, lymphocytes, eosinophils, neutrophils) between the tazanolast-treated sham group and the vehicle-treated sham group.
Chemical Information
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No. CAS 82989-25-1
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Appearance Solid
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Peso molecular 289.29
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Fòrmula C13H15N5O3
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Color White to off-white
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SMILES
O=C(OCCCC)C(NC1=CC=CC(C2=NN=NN2)=C1)=O
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Synonyms
TO 188; Tazalest; Tazanol
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (345.67 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. 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)
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 (8.64 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.
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.
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 (281 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Igarashi A, et al. Tazanolast inhibits ozone-induced airway hyperresponsiveness in guinea pigs. Am J Respir Crit Care Med. 1998 May;157(5 Pt 1):1531-5. [Content Brief]
[3]. Csaba G, et al. Prolonged effect of an H1-receptor blocker antihistamine on the histamine content of white blood cells and mast cells. Cell Biochem Funct. 2004 May-Jun;22(3):201-4. [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. 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 | 3.4567 mL | 17.2837 mL | 34.5674 mL | 86.4185 mL |
| 5 mM | 0.6913 mL | 3.4567 mL | 6.9135 mL | 17.2837 mL | |
| 10 mM | 0.3457 mL | 1.7284 mL | 3.4567 mL | 8.6418 mL | |
| 15 mM | 0.2304 mL | 1.1522 mL | 2.3045 mL | 5.7612 mL | |
| 20 mM | 0.1728 mL | 0.8642 mL | 1.7284 mL | 4.3209 mL | |
| 25 mM | 0.1383 mL | 0.6913 mL | 1.3827 mL | 3.4567 mL | |
| 30 mM | 0.1152 mL | 0.5761 mL | 1.1522 mL | 2.8806 mL | |
| 40 mM | 0.0864 mL | 0.4321 mL | 0.8642 mL | 2.1605 mL | |
| 50 mM | 0.0691 mL | 0.3457 mL | 0.6913 mL | 1.7284 mL | |
| 60 mM | 0.0576 mL | 0.2881 mL | 0.5761 mL | 1.4403 mL | |
| 80 mM | 0.0432 mL | 0.2160 mL | 0.4321 mL | 1.0802 mL | |
| 100 mM | 0.0346 mL | 0.1728 mL | 0.3457 mL | 0.8642 mL |
Tazanolast Related Classifications
HY-101810 Related Classifications
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Keywords
- Tazanolast
- 82989-25-1
- TO 188
- Tazalest
- Tazanol
- TO188
- TO-188
- Calcium Channel
- PKC
- intracellular calcium concentration
- passive cutaneous anaphylaxis
- Schultz-Dale reaction
- protein kinase C translocation
- experimental asthma
- histamine release
- guinea pigs
- mast cells
- inositol trisphosphate
- substance P
- Inhibitor
- inhibitor
- inhibit