| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| 100mg | |||
| Other Sizes |
| Targets |
Quinotolast sodium acts by inhibiting mast cell degranulation and reducing the release of histamine and other inflammatory mediators. It exerts its effects by stabilizing mast cells, preventing the release of allergic mediators such as histamine, LTC4, and PGD2.
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| ln Vitro |
In dispersed human lung cells, quinotolast inhibits the release of histamine as well as the production of prostaglandin D2 and leukotriene (LT) C4. Quinotolast (100 μg/mL) markedly reduced 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 was largely independent of the preincubation period, and no tachyphylaxis was observed. Quinotolast has a significant inhibitory effect on inflammatory mediators in human dispersed lung cells [1]. Quinotolast also showed strong inhibitory effects on histamine and the peptide leukotrienes released from guinea pig lung fragments or mouse cultured mast cells. Quinotolast concentration-dependently inhibits pLT release from cultured mast cells. The IC50 value of Quinotolast is 0.72 μg/mL[2].
In vitro, Quinotolast sodium has a significant inhibitory effect on inflammatory mediators in human dispersed lung cells. It also shows strong inhibitory effects on histamine and peptide leukotrienes released from guinea pig lung fragments or mouse cultured mast cells. It inhibits histamine, LTC4, and PGD2 in the concentration range of 1-100 microg/mL. |
| ln Vivo |
Quinotolast can effectively suppress type I allergic reactions, including allergic bronchoconstriction and passive cutaneous anaphylaxis (PCA), in rats when administered intravenously and orally. When given intravenously to rats, quinotolast inhibits PCA in a dose-dependent manner. 0.0063 mg/kg of quinolast is the dose needed to suppress the response by 50% (ED50). When taken orally, quinotolast suppresses this reaction. Quinlilast's ED50 value is 0.0081 mg/kg. At a dose of 0.32 mg/kg, Quinotolast almost completely inhibited, but at a dose of 1 mg/kg, its effect was somewhat diminished [2].
In vivo, Quinotolast sodium has been studied for its potential in treating asthma and allergic rhinitis. As a mast cell stabilizer, it is expected to reduce the symptoms of allergic reactions by preventing the release of inflammatory mediators. |
| Enzyme Assay |
In vitro assays for Quinotolast sodium involve measuring its effects on mast cell degranulation and mediator release. Mast cells are treated with the compound and stimulated with an allergen or other trigger. The release of histamine, LTC4, and PGD2 is measured to assess its inhibitory activity.
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| Cell Assay |
Cellular assays for Quinotolast sodium are conducted using mast cells or lung cells. Cells are treated with the compound and stimulated, and the release of inflammatory mediators such as histamine and leukotrienes is measured.
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| Animal Protocol |
In vivo animal studies for Quinotolast sodium are conducted in models of allergic asthma and rhinitis. Animals are treated with the compound, and endpoints such as airway inflammation, nasal symptoms, and mediator levels are assessed to evaluate its efficacy.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Quinotolast sodium are characteristic of a small molecule. It has a molecular weight of 371.31 and a molecular formula of C17H12N6NaO3. It is a sodium salt and is typically stored as a solid.
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| Toxicity/Toxicokinetics |
The toxicological profile of Quinotolast sodium is not fully detailed. As an antiallergic agent, its safety has been evaluated in preclinical and clinical studies. It is for research use only and is not for therapeutic use.
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| References | |
| Additional Infomation |
Quinotolast sodium is an antiallergic agent and mast cell stabilizer. It has been studied for asthma and allergic rhinitis. It inhibits histamine, LTC4, and PGD2 release and is available for research use only.
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| Molecular Formula |
C17H11N6NAO3
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| Molecular Weight |
370.297413110733
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| Exact Mass |
371.087
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| CAS # |
101193-62-8
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| PubChem CID |
14600474
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
1.93
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
726
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CDPWRMHFRRXOQH-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C17H12N6O3.Na/c24-15(18-17-19-21-22-20-17)12-10-14(26-11-6-2-1-3-7-11)13-8-4-5-9-23(13)16(12)25;/h1-10H,(H2,18,19,20,21,22,24);/q;+1/p-1
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| Chemical Name |
sodium;4-oxo-1-phenoxy-N-(1,2,3-triaza-4-azanidacyclopenta-2,5-dien-5-yl)quinolizine-3-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~115 mg/mL (~309.71 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 5.75 mg/mL (15.49 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 57.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 5.75 mg/mL (15.49 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 57.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7005 mL | 13.5026 mL | 27.0051 mL | |
| 5 mM | 0.5401 mL | 2.7005 mL | 5.4010 mL | |
| 10 mM | 0.2701 mL | 1.3503 mL | 2.7005 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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