Quinotolast sodium
Based on 1 Customer Validation
Quinotolast sodium in the concentration range of 1-100 μg/mL inhibits histamine, LTC4 and PGD2 release in a concentration-dependent manner.
For research use only. We do not sell to patients.
- Purity: 98.38%
- CAS No.: 101193-62-8
- Formula: C17H12N6NaO3
- Molecular Weight:371.31
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Storage:
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Histamine |
LTC4 |
Quinotolast inhibits the release of histamine and the generation of leukotriene (LT) C4 and prostaglandin (PG) D2 from dispersed human lung cells. Quinotolast (100 μg/mL) significantly inhibits PGD2 and LTC4 release. Quinotolast inhibits PGD2 release by 100% and LTC4 release by 54%. The inhibitory effect of Quinotolast on histamine release from dispersed lung cells is largely independent of the preincubation period, no tachyphylaxis being observed. Quinotolast shows a significant inhibition of inflammatory mediators from human dispersed lung cells[1]. Quinotolast also shows strong inhibitory effects on histamine and peptide leukotrienes release from guinea pig lung fragments or mouse cultured mast cells. Quinotolast concentration-dependently inhibits pLTs release from cultured mast cells. The IC50 value for Quinotolast is 0.72 μg/mL[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 101193-62-8
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Appearance Solid
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Molecular Weight 371.31
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Formula C17H12N6NaO3
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Color Light yellow to yellow
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SMILES
O=C(NC1=NN=NN1)C2=CC(OC3=CC=CC=C3)=C4N(C2=O)C=CC=C4.[Na]
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Synonyms
FR71021
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 115 mg/mL (309.71 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)
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: 5.75 mg/mL (15.49 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5.75 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (57.5 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: 5.75 mg/mL (15.49 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5.75 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (57.5 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.
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.
Protocol
Mast cells are obtained after the culture of bone marrow cells from the femurs of female BDF1 mice in the presence of conditioned medium from WEHI-3 cells containing interleukin 3. The cells are suspended with Tyrode's buffer (137 mM NaCI, 2.7 mM KC1, 1.8 mM CaCl2, 1 mM MgCl2, 0.4 mM NaH2PO4, 11.9 mM NaHCO3, 5.6 mM glucose) containing 0.1% gelatin and are sensitized with mouse monoclonal anti-DNP IgE (50 μg/106 cells). Then the cells are washed and resuspended with Tyrode's buffer containing 0.25% BSA. The cells (2×106 cells) are incubated for 5 min at
37°C and challenged with TNP-BSA (2 ng BSA/mL). Quinotolast (0.1, 1, 10, 100 ug/mL) is added to the reaction tube simultaneously with the antigen. Ten minutes later, the reaction is stopped by the addition of EDTA (2.7 mM). pLTs in the cell supernatant sre quantified as immunoreactive leukotriene C4 (iLTC4) with a leukotriene C4/D4/E4[3H] assay system. % Inhibition is calculated in each experiment from the amount of immunoreactive leukotriene C4 (iLTC4)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats [2]
Rats (8 week-old) are used. To study the presence of tachyphylaxis by Quinotolast, Quinotolast (0.001, 0.01, 0.1, 1,10 and 100 mg/kg) is given i.v. in a large dose 30 min before challenge, and again at a smaller dose simultaneously with the antigen challenge.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (281 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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Handling Instructions (2659 KB)
References
[1]. Okayama Y, et al. Inhibition of histamine and eicosanoid release from dispersed human lung cells in vitro byquinotolast. Jpn J Pharmacol. 1995 Dec;69(4):375-80. [Content Brief]
[2]. Kobayashi K, et al. Effects of quinotolast, a new orally active antiallergic drug, on experimental allergic models. Jpn J Pharmacol. 1993 Sep;63(1):73-81. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6932 mL | 13.4658 mL | 26.9317 mL | 67.3292 mL |
| 5 mM | 0.5386 mL | 2.6932 mL | 5.3863 mL | 13.4658 mL | |
| 10 mM | 0.2693 mL | 1.3466 mL | 2.6932 mL | 6.7329 mL | |
| 15 mM | 0.1795 mL | 0.8977 mL | 1.7954 mL | 4.4886 mL | |
| 20 mM | 0.1347 mL | 0.6733 mL | 1.3466 mL | 3.3665 mL | |
| 25 mM | 0.1077 mL | 0.5386 mL | 1.0773 mL | 2.6932 mL | |
| 30 mM | 0.0898 mL | 0.4489 mL | 0.8977 mL | 2.2443 mL | |
| 40 mM | 0.0673 mL | 0.3366 mL | 0.6733 mL | 1.6832 mL | |
| 50 mM | 0.0539 mL | 0.2693 mL | 0.5386 mL | 1.3466 mL | |
| 60 mM | 0.0449 mL | 0.2244 mL | 0.4489 mL | 1.1222 mL | |
| 80 mM | 0.0337 mL | 0.1683 mL | 0.3366 mL | 0.8416 mL | |
| 100 mM | 0.0269 mL | 0.1347 mL | 0.2693 mL | 0.6733 mL |
Quinotolast sodium Related Classifications
HY-U00027 Related Classifications
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