Pemirolast potassium

Catalog No.S4008

Pemirolast potassium (BMY 26517) is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent.

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Pemirolast potassium Chemical Structure

Pemirolast potassium Chemical Structure
Molecular Weight: 266.3

Validation & Quality Control

Quality Control & MSDS

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Product Description

Biological Activity

Description Pemirolast potassium (BMY 26517) is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent.
Targets Histamine H1 receptor [2]
In vitro Pemirolast potassium (BMY 26517) is a new oral, nonbronchodilator antiallergy medication that is being evaluated for the therapy of asthma. [1] Pemirolast potassium (BMY 26517) inhibits chemical mediator release from tissue mast cells and is also shown to inhibit the release of peptides including substance P, [2] neurokinin (NK) A, and calcitonin gene-related peptide (CGRP) from sensory nerves. [3] Pemirolast potassium is used for the treatment of allergic conjunctivitis and prophylaxis for pulmonary hypersensitivity reactions to drugs such as paclitaxel. [4]
In vivo Pemirolast potassium (BMY 26517) reduces kaolin intake by inhibition of substance P release in rats. [2] Pemirolast potently attenuates paclitaxel hypersensitivity reactions through inhibition of the release of sensory neuropeptides in rats. [3]
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Kemp JP, et al. Ann Allergy, 1992, 68(6), 488-491.

[2] Tatsushima Y, et al. Eur J Pharmacol, 2011, 661(1-3), 57-62.

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Chemical Information

Download Pemirolast potassium SDF
Molecular Weight (MW) 266.3
Formula

C10H7N6O.K

CAS No. 100299-08-9
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms BMY26517
Solubility (25°C) * In vitro Water 53 mg/mL (199.02 mM)
DMSO <1 mg/mL
Ethanol <1 mg/mL
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 4H-Pyrido[1,2-a]pyrimidin-4-one, 9-methyl-3-(2H-tetrazol-5-yl)-, potassium salt (1:1)

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