Zileuton

Catalog No.S1443 Synonyms: A-64077

Zileuton Chemical Structure

Molecular Weight(MW): 236.29

Zileuton is an orally active inhibitor of 5-lipoxygenase, and thus inhibits leukotrienes (LTB4, LTC4, LTD4, and LTE4) formation, used to decrease the symptoms of asthma.

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock
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1 Customer Review

  • CD19+ B cells (A) or PBMCs (B) from a healthy donor were treated with zileuton (10 μM) prior to 17-HDHA or RvD1 treatment, followed by stimulation with the IgE-inducing cocktail. Cell culture supernatants were collected at day 7, and IgE levels were measured. The experiment was done in one representative donor (mean ± SEM). Data were analyzed by 1-way ANOVA with Tukey’s post test, **P ≤ 0.01, ***P ≤ 0.001. PBMC, peripheral blood mononuclear cell.

    JCI Insight, 2017, 2(3):e88588. Zileuton purchased from Selleck.

Purity & Quality Control

Choose Selective Lipoxygenase Inhibitors

Biological Activity

Description Zileuton is an orally active inhibitor of 5-lipoxygenase, and thus inhibits leukotrienes (LTB4, LTC4, LTD4, and LTE4) formation, used to decrease the symptoms of asthma.
Targets
5-lipoxygenase [1]
In vitro

Zileuton suppresses PG biosynthesis by interference with arachidonic acid (AA) release in macrophages. Zileuton significantly reduces PGE2 and 6-keto prostaglandin F1α (PGF1α) levels in activated mouse peritoneal macrophages and in J774 macrophages. Zileuton inhibits PGE2 production in LPS-stimulated human whole blood and suppresses PGE2 and 6-keto PGF1α pleural levels in rat carrageenan-induced pleurisy. [1]

In vivo Zileuton significantly reduces macroscopic damage score after four weeks of treatment in rats. Zileuton administration significantly increases the intracolonic release of both thromboxane B2 at week 1 and prostaglandin E2 at weeks 2 and 4 in rats. [2] Zileuton reduces the spinal cord inflammation and tissue injury, neutrophil infiltration, TNF-alpha, COX-2 and pERK1/2 expression, PGE(2) and LTB(4) production, and apoptosis in mice. Zileuton significantly improves the recovery of limb function over 10 days in mice.[3]

Zileuton administrated before I/R significantly reduces the degree of renal dysfunction (urea, creatinine) and injury (AST, histology) in 5-lipoxygenase knockout mice. Zileuton reduces the expression of ICAM-1 and the associated PMN infiltration caused by I/R of the mouse kidney in 5-lipoxygenase knockout mice. [4]

Zileuton inhibits LTB(4) production in the peritonitis model more effectively than the LTA(4)H inhibitor, but the influx of neutrophils into the peritoneum after 1 and 2 hours is significantly higher in Zileuton- versus JNJ-26993135-treated mice. [5]

Protocol

Solubility (25°C)

In vitro DMSO 47 mg/mL (198.9 mM)
Ethanol 47 mg/mL (198.9 mM)
Water 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 Information

Molecular Weight 236.29
Formula

C11H12N2O2S

CAS No. 111406-87-2
Storage powder
Synonyms A-64077

Bio Calculators

Molarity Calculator

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02348203 Recruiting Pulmonary Nodules|Tobacco Use Disorder National Cancer Institute (NCI) January 2016 Phase 2
NCT02047149 Terminated Chronic Myelogenous Leukemia University of Massachusetts, Worcester|Bristol-Myers Squibb January 2014 Phase 1
NCT01805687 Completed Asthma Cornerstone Therapeutics Inc. March 2013 Phase 4
NCT01174056 Completed Lung Inflammation Washington University School of Medicine|Doris Duke Charitable Foundation July 2011 Early Phase 1
NCT01136941 Completed Sickle Cell Disease Childrens Hospital Medical Center, Cincinnati September 2010 Phase 1
NCT01021215 Completed Tobacco Use Disorder National Cancer Institute (NCI) May 2010 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID