Pemirolast potassium
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Pemirolast potassium is an orally active antiallergic agent. Pemirolast potassium attenuates Paclitaxel (HY-B0015) hypersensitivity reactions. Pemirolast potassium can be used for bronchial asthma and conjunctivitis research-.
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- Pureza: 99.99%
- No. CAS: 100299-08-9
- Fòrmula: C10H7KN6O
- Peso molecular:266.30
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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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Ver todos los productos específicos de isoformas Histamine Receptor
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Actividad biológica
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H1 Receptor |
Pemirolast (1 μM-1 mM) potassium inhibits A23187-induced LTC4 and ECP release from the eosinophils in a dose-dependent manner[1].
Pemirolast (0.1-1 mM) potassium also inhibits PAF-induced and FMLP-induced ECP release from the eosinophils[1].
Pemirolast potassium prevents the activation of human eosinophils to inhibit granule protein LTQ and ECP release, so that alleviates controlling allergic diseases[1].
Pemirolast (100 nM-1 mM; 1-15 min) potassium fails to significantly inhibit histamine release from human conjunctival mast cells[2].
Pemirolast (0.1 μg/mL-0.01 mg/mL) potassium inhibits the activation of signal transduction phospholipases C and AZ in rat peritoneal mast cells, by inhibiting the degranulation reaction of antigen and compound 48/80, suppressing the formation of 1,2-diacylglycerol and phosphatidylic acid[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pemirolast (0.1-1 mg/kg; i.v.) potassium inhibits taxel-induced pulmonary vascular hyperpermeability, and reverses paclitaxel-induced arterial PaO2 decreasing at a dosage of 1 mg/kg, 30 minutes after paclitaxel (HY-B0015) injection (15 mg/kg; i.v.)[4].
Pemirolast (10 mg/kg/d; p.o.; 4-5 d) potassium significantly reduces Cisplatin (HY-17394)-induced kaolin intake on days 3 and 4 and inhibits cisplatin-induced substance P release in the cerebrospinal fluid (CSF) in rats[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats (6-week-old, 160-250 g)[5]
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Dosage:10 mg/kg
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Administration:Oral gavage; 4 days: 30 min before and 24, 48, 72 and 96 h (four times in total) after administration of cisplatin (5 mg/kg; i.v.).
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Result:Significantly reversed the cisplatin-induced increase of substance P levels to vehicle levels in the CSF.
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Animal Model:Male Wistar rats (6-week-old, 160-250 g)[5]
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Dosage:10 mg/kg
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Administration:Oral gavage; 5 days: 1 h or 30 min before and 24, 48, 72 and 96 h (five times in total) after administration of cisplatin (2-10 mg/kg; i.v.)
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Result:Inhibited the cisplatin-induced increase in kaolin intake on days 3 and 4, without decreasing in normal feed intake.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 100299-08-9
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Appearance Solid
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Peso molecular 266.30
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Fòrmula C10H7KN6O
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Color Light yellow to green yellow
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SMILES
O=C1C(C2=N[N-]N=N2)=CN=C3N1C=CC=C3C.[K+]
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Synonyms
TWT-8152; BMY 26517
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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 : 50 mg/mL (187.76 mM; Need ultrasonic)
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)
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 (375.52 mM); Clear solution; Need ultrasonic
Pureza y Documentación
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Ficha de datos (276 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]. Kawashima T, et al. Inhibitory effect of pemirolast, a novel antiallergic drug, on leukotriene C4 and granule protein release from human eosinophils. Int Arch Allergy Immunol. 1994;103(4):405-9. [Content Brief]
[2]. Yanni JM, et al. Comparative effects of topical ocular anti-allergy drugs on human conjunctival mast cells. Ann Allergy Asthma Immunol. 1997 Dec;79(6):541-5. [Content Brief]
[3]. Fujimiya H, et al. Effect of a novel antiallergic drug, pemirolast, on activation of rat peritoneal mast cells: inhibition of exocytotic response and membrane phospholipid turnover. Int Arch Allergy Appl Immunol. 1991;96(1):62-7. [Content Brief]
[4]. Itoh Y, et al. Pemirolast potently attenuates paclitaxel hypersensitivity reactions through inhibition of the release of sensory neuropeptides in rats. Neuropharmacology. 2004 May;46(6):888-94. [Content Brief]
[5]. Tatsushima Y, et al. Pemirolast reduces cisplatin-induced kaolin intake in rats. Eur J Pharmacol. 2011 Jul 1;661(1-3):57-62. [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 | 1 mM | 3.7552 mL | 18.7758 mL | 37.5516 mL | 93.8791 mL |
| 5 mM | 0.7510 mL | 3.7552 mL | 7.5103 mL | 18.7758 mL | |
| 10 mM | 0.3755 mL | 1.8776 mL | 3.7552 mL | 9.3879 mL | |
| 15 mM | 0.2503 mL | 1.2517 mL | 2.5034 mL | 6.2586 mL | |
| 20 mM | 0.1878 mL | 0.9388 mL | 1.8776 mL | 4.6940 mL | |
| 25 mM | 0.1502 mL | 0.7510 mL | 1.5021 mL | 3.7552 mL | |
| 30 mM | 0.1252 mL | 0.6259 mL | 1.2517 mL | 3.1293 mL | |
| 40 mM | 0.0939 mL | 0.4694 mL | 0.9388 mL | 2.3470 mL | |
| 50 mM | 0.0751 mL | 0.3755 mL | 0.7510 mL | 1.8776 mL | |
| 60 mM | 0.0626 mL | 0.3129 mL | 0.6259 mL | 1.5647 mL | |
| 80 mM | 0.0469 mL | 0.2347 mL | 0.4694 mL | 1.1735 mL | |
| 100 mM | 0.0376 mL | 0.1878 mL | 0.3755 mL | 0.9388 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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