Pemirolast

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Pemirolast is an orally active antiallergic agent. Pemirolast attenuates paclitaxel hypersensitivity reactions, can be used for bronchial asthma and conjunctivitis research^-.

For research use only. We do not sell to patients.

Pemirolast Chemical Structure

CAS No. : 69372-19-6

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Purity & Documentation
References
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Description

Pemirolast is an orally active antiallergic agent. Pemirolast attenuates paclitaxel hypersensitivity reactions, can be used for bronchial asthma and conjunctivitis research^[1]^-^[5].

In Vitro

Pemirolast (1 μM-1 mM) inhibits A23187-induced LTC4 and ECP release from the eosinophils in a dose-dependent manner^[1].
Pemirolast (0.1 mM and 1 mM) also inhibits PAF-induced and FMLP-induced ECP release from the eosinophils^[1].
Pemirolast 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) fails to significantly inhibit histamine release from human conjunctival mast cells^[2].
Pemirolast (0.1 μg/mL-0.01 mg/mL) 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.

In Vivo

Pemirolast potently attenuates paclitaxel hypersensitivity reactions through inhibition of the release of sensory neuropeptides in rats^[4].
Pemirolast (0.1-1 mg/kg; i.v.) inhibits taxel-induced pulmonary vascular hyperpermeability, and reverses paclitaxel-induced arterial PaO2 decreasing at a dosage of 1 mg/kg, 30 minutes after paclitaxel injection (15 mg/kg; i.v.)^[4].
Pemirolast (1 mg/kg; i.v.) reverses taxel-induced elevation of the concentrations of sensory neuropeptides (CGRP, substance P and neurokinin A), 30 minutes after paclitaxel injection (15 mg/kg; i.v.)^[4].
Pemirolast (10 mg/kg/d; p.o.; 4-5 d) significantly reduces cisplatin-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.

Animal Model:	Male Wistar rats (6-week-old, 160-250 g)^[5]
Dosage:	10 mg/kg
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.)
Result:	Inhibited the cisplatin-induced increase in kaolin intake on days 3 and 4, without decreasing in normal feed intake.

Animal Model:	Male Wistar rats (6-week-old, 160-250 g)^[5]
Dosage:	10 mg/kg
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.).
Result:	Significantly reversed the cisplatin-induced increase of substance P levels to vehicle levels in the CSF.

Clinical Trial

Molecular Weight

228.21

Formula

C₁₀H₈N₆O

CAS No.

69372-19-6

SMILES

O=C1C(C2=NNN=N2)=CN=C3N1C=CC=C3C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (438.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

DMF : < 1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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mg/kg

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Handling Instructions (2659 KB)

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. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	4.3819 mL	21.9096 mL	43.8193 mL	109.5482 mL
	5 mM	0.8764 mL	4.3819 mL	8.7639 mL	21.9096 mL
	10 mM	0.4382 mL	2.1910 mL	4.3819 mL	10.9548 mL
	15 mM	0.2921 mL	1.4606 mL	2.9213 mL	7.3032 mL
	20 mM	0.2191 mL	1.0955 mL	2.1910 mL	5.4774 mL
	25 mM	0.1753 mL	0.8764 mL	1.7528 mL	4.3819 mL
	30 mM	0.1461 mL	0.7303 mL	1.4606 mL	3.6516 mL
	40 mM	0.1095 mL	0.5477 mL	1.0955 mL	2.7387 mL
	50 mM	0.0876 mL	0.4382 mL	0.8764 mL	2.1910 mL
	60 mM	0.0730 mL	0.3652 mL	0.7303 mL	1.8258 mL
	80 mM	0.0548 mL	0.2739 mL	0.5477 mL	1.3694 mL
	100 mM	0.0438 mL	0.2191 mL	0.4382 mL	1.0955 mL

Pemirolast Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pemirolast69372-19-6Othershuman eosinophilsleukotriene C4granule proteinsubstance Pcerebrospinal fluidCSFkaolin intakevomitInhibitorinhibitorinhibit

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