Pemirolast potassium (Synonyms: TWT-8152; BMY 26517)

Cat. No.: HY-B0538A Purity: 99.99%: Data Sheet
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Handling Instructions
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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^-.

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

Pemirolast potassium Chemical Structure

CAS No. : 100299-08-9

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in Water	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
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Other Forms of Pemirolast potassium:

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H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

H₁ Receptor

In Vitro

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.

In Vivo

Pemirolast potassium potently attenuates Paclitaxel hypersensitivity reactions through inhibition of the release of sensory neuropeptides in rats^[4].
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.

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.

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.

Clinical Trial

Molecular Weight

266.30

Formula

C₁₀H₇KN₆O

CAS No.

100299-08-9

Appearance

Solid

Color

Light yellow to green yellow

SMILES

O=C1C(C2=N[N-]N=N2)=CN=C3N1C=CC=C3C.[K+]

Shipping

Room temperature in continental US; may vary elsewhere.

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

In Vitro:

H₂O : 50 mg/mL (187.76 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.7552 mL	18.7758 mL	37.5516 mL
5 mM	0.7510 mL	3.7552 mL	7.5103 mL
10 mM	0.3755 mL	1.8776 mL	3.7552 mL

View the 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.

* 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

Add each solvent one by one: PBS
Solubility: 100 mg/mL (375.52 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.99%

Select Batch:

Data Sheet (276 KB) SDS (392 KB)

COA (250 KB) HNMR (136 KB) LCMS (93 KB)

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

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.

Pemirolast potassium Related Classifications

Inflammation/Immunology Cardiovascular Disease

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:

Pemirolast100299-08-9TWT-8152 BMY 26517TWT8152TWT 8152BMY26517BMY 26517BMY-26517Histamine ReceptorratsCSFhyperpermeabilityeosinophilsallergic diseasesInhibitorinhibitorinhibit

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