Pranlukast

Catalog No.S1829 Batch:S182902

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Technical Data

Formula

C27H23N5O4

Molecular Weight 481.5 CAS No. 103177-37-3
Solubility (25°C)* In vitro DMSO 48 mg/mL (99.68 mM)
Water Insoluble
Ethanol Insoluble
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Pranlukast (ONO-1078,ono-rs-411) is an orally administered, and selective antagonist of the cysteinyl leukotrienes (LT) C(4), LTD(4) and LTE(4), used in the prophylactic treatment of chronic bronchial asthma.
Targets
Cysteinyl leukotriene [1]
In vitro

Pranlukast inhibits NF-kappa B activation in 1.3% DMSO-differentiated U-937 and Jurkat cells by about 40% & 30%, respectively. Pranlukast and MK-571 inhibit NF-kappa B activation in 1.3% DMSO-differentiated U-937 and Jurkat cells in a dose-related manner. Pranlukast and MK-571 inhibits LPS-induced IL-6 production in PBMC by about 65% and 15%, respectively. [1] Pranlukast or zafirlukast significantly inhibits 10 mM LTD4-evoked 35SO4 output in a concentration-dependent fashion, with maximal inhibitions of 83% at 10 mM Pranlukast and 78% at 10 mM Zafirlukast, and IC50 values of 0.3 mM for Pranlukast and 0.6 mM for Zafirlukast. Pranlukast (0.5 microM) causes a parallel rightward shift of the LTD4 concentration-response curve with a pKB of 7. Pranlukast or Zafirlukast (5 microM each) significantly suppresses ovalbumin-induced secretion in tracheae from sensitized guinea-pigs by 70% and 65%, respectively. [2] Pranlukast also inhibits NF-kappaB activation induced by phorbol 12-myristate 13-acetate (PMA). Pranlukast also significantly inhibits LPS-induced MUC2 mRNA expression by reverse transcription-polymerase chain reaction (RT-PCR) analysis in NCI-H292 cells. Pranlukast also inhibits LPS-induced MUC2 gene expression in HM3-MUC2 cells. [3]

In vivo

Pranlukast significantly reduces lesion volume, and increases neuron densities in the cortex and hippocampal CA1 region in the ischemic hemispheres of mice. Pranlukast also remarkably reduces the thickness of a scar wall in the ischemic hemispheres of mice. [4]

Protocol (from reference)

Selleck's Pranlukast has been cited by 1 publication

Leukotriene receptor antagonists enhance HCC treatment efficacy by inhibiting ADAMs and suppressing MICA shedding [ Cancer Immunol Immunother, 2021, 70(1):203-213] PubMed: 32683508

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.