| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg |
| ln Vitro |
A23187-induced LTC4 and ECP release from eosinophils is dose-dependently inhibited by pemirolast (1 μM-1 mM) [1]. Pemirolast (0.1 mM and 1 mM) also prevents eosinophil ECP release that is triggered by FMLP and PAF [1]. By limiting human eosinophil activation, pirazolast reduces the production of granular proteins LTQ and ECP, which helps to alleviate and regulate allergic disorders [1]. Human conjunctival mast cells' histamine production is not substantially inhibited by pemirolast (100 nM-1 mM; 1–15 minutes) [2]. Pemirolast (0.1 μg/mL-0.01 mg/mL) suppresses the production of 1,2-diacylglycerol and the degranulation reaction of antigen and compound 48/80 in rat peritoneal mast cells, thereby inhibiting the signal transmission phospholipase C. and phosphatidyl acid and AZ activation [3].
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| ln Vivo |
Pemirolast blocks rats' release of sensory neuropeptides, which effectively reduces paclitaxel allergic reactions [4]. Half an hour after starting paclitaxel (15 mg/kg; i.v.) at a dose of 1 mg/kg, pemirolast (0.1-1 mg/kg; i.v.) inhibits and reverses the decrease in arterial PaO2 caused by paclitaxel-induced pulmonary vascular hyperpermeability. 4]. Thirty minutes after paclitaxel injection (15 mg/kg; iv), pemirolast (1 mg/kg; iv) reverses the increases in sensory neuropeptide (CGRP, substance P, and neurokinin A) concentrations caused by paclitaxel [4]. Pemirolast (10 mg/kg/d; oral; days 4-5) inhibits the release of substance P in rat cerebrospinal fluid (CSF) induced by cisplatin and significantly reduces kaolin intake on days 3 and 4[5].
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| Animal Protocol |
Animal/Disease Models: Male Wistar rats (6 weeks old, 160-250 g) [5]
Doses: 10 mg/kg Route of Administration: po (oral gavage); 5 days: 1 hour or 30 minutes before and after cisplatin administration Experimental Results: Inhibition of cisplatin-induced increase in kaolin intake at 24, 48, 72 and 96 hrs (hrs (hours)) (5 times in total) (2-10 mg/kg; iv) on days 3 and 4 without reduction in normal feed intake . Animal/Disease Models: Male Wistar rats (6 weeks old, 160-250 g) [5] Doses: 10 mg/kg Route of Administration: po (oral gavage); 4 days: 30 days before cisplatin (5 mg/kg; iv) administration minutes and 24, 48, 72 and 96 hrs (hrs (hours)) after dosing (four times in total). Experimental Results: Significant reversal of cisplatin-induced elevation of substance P levels in cerebrospinal fluid to vehicle levels. |
| References |
[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.
[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. [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. [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. [5]. Tatsushima Y, et al. Pemirolast reduces cisplatin-induced kaolin intake in rats. Eur J Pharmacol. 2011 Jul 1;661(1-3):57-62. |
| Molecular Formula |
C10H8N6O
|
|---|---|
| Molecular Weight |
228.21012
|
| CAS # |
69372-19-6
|
| Related CAS # |
Pemirolast potassium;100299-08-9
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
CC1=CC=CN2C(C(C3=NNN=N3)=CN=C12)=O
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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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~438.19 mM)
DMF :< 1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.3819 mL | 21.9096 mL | 43.8193 mL | |
| 5 mM | 0.8764 mL | 4.3819 mL | 8.7639 mL | |
| 10 mM | 0.4382 mL | 2.1910 mL | 4.3819 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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