Zileuton sodium

"目录号: HY-14164A

Metabolic Enzyme/Protease-

Zileuton sodium 是一种有效的，选择性的5-lipoxygenase抑制剂，具有抗炎的作用。

5-Lipoxygenase

相关产品

U-73122-Zileuton-ML355-Enazadrem-LY 178002-Malotilate-RWJ 63556-S-2474-CMI-392-CMI977-PGS-IN-1-RS4317-S-(+)-Marmesin-U66858-

生物活性

Description

Zileuton sodium is a potent and selective inhibitor of5-lipoxygenase, exhibiting inflammatory activities.

In Vitro

In anti-CD3-treated cells, IL-2 decreases in zileuton-treated and untreated cells with increasing incubation time. Zileuton likely reduces IL-2 levels by inhibiting 5-lipoxygenase, hence leukotriene B4 production, an IL-2 inducer[2].

In Vivo

In zileuton (5 mg/kg, p.o.) treated I/R rat, the effect of zileuton to decrease NF-κB expression does not change significantly in the presence of COX inhibitors, and the group reveals significantly lower level of NF-κB staining. Zileuton (5 mg/kg, p.o.) treatment given to I/R rats decreases apoptotic index significantly. Zileuton has no significant effect on increased serum TNF-α levels in I/R group[1]. Zileuton (1200 mg/kg) inhibits the polyp formation in APCΔ468colon and small intestine. Zileuton treatment inhibits the proliferation rates of non epithelial cells in polyps, and increases the apoptosis rates in polyps in rat. There is significant increase in the number of apoptotic cells in the Zileuton-treated cells both in small intestine and in the colon. The reduced proliferation rate may significantly contribute to the reduction of polyposis in both the small intestine and colon of Zileuton-fed APCΔ468mice[3].

Clinical Trial

NCT01136941

Children's Hospital Medical Center, Cincinnati

Sickle Cell Disease

September 2010

Phase 1

NCT01130688

University of Massachusetts, Worcester

Chronic Myelogenous Leukemia

January 2010

Phase 1

NCT02047149

University of Massachusetts, Worcester-Bristol-Myers Squibb

Chronic Myelogenous Leukemia

January 2014

Phase 1

NCT00575861

Gelb, Arthur F., M.D.

Asthma

September 2005

Phase 4

NCT00486343

Critical Therapeutics

Asthma

July 2007

Phase 4

NCT02348203

National Cancer Institute (NCI)

Pulmonary Nodules-Tobacco Use Disorder

January 13, 2016

Phase 2

NCT00262405

University of Michigan-National Institutes of Health (NIH)

Idiopathic Pulmonary Fibrosis

January 2001

Phase 2

NCT00534625

Critical Therapeutics

Asthma

September 2007

Phase 2

NCT00493974

University of Minnesota - Clinical and Translational Science Institute-National Heart, Lung, and Blood Institute (NHLBI)

Pulmonary Disease, Chronic Obstructive

March 2007

Phase 3

NCT00056004

Barbara Ann Karmanos Cancer Institute-National Cancer Institute (NCI)

Head and Neck Cancer-Lung Cancer

June 2003

Phase 2

NCT01021215

National Cancer Institute (NCI)

Tobacco Use Disorder

May 2010

Phase 1-Phase 2

NCT00098358

Critical Therapeutics

Acne Vulgaris

November 2004

Phase 2

NCT00299065

Critical Therapeutics

Asthma

January 2006

Phase 1-Phase 2

NCT01805687

Cornerstone Therapeutics Inc.

Asthma

March 2013

Phase 4

NCT00070486

Alliance for Clinical Trials in Oncology-National Cancer Institute (NCI)

Lung Cancer

December 2003

Phase 2

NCT01174056

Washington University School of Medicine-Doris Duke Charitable Foundation

Lung Inflammation

July 2011

Early Phase 1

NCT00467831

National Human Genome Research Institute (NHGRI)-National Institutes of Health Clinical Center (CC)

Hermansky-Pudlak Syndrome (HPS)-Pulmonary Fibrosis-Oculocutaneous Albinism-Platelet Storage Pool Deficiency-Metabolic Disease

April 2007

Phase 1-Phase 2

NCT00723021

Pfizer

Asthma

July 2008

Phase 2

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References

[1].Abueid L, et al. Inhibition of 5-lipoxygenase by zileuton in a rat model of myocardial infarction. Anatol J Cardiol. 2016 Nov 10.

[2].Kuvibidila S, et al. Hydroxyurea and Zileuton Differentially Modulate Cell Proliferation and Interleukin-2 Secretion by Murine Spleen Cells: Possible Implication on the Immune Function and Risk of Pain Crisis in Patients with Sickle Cell Disease. Ochsner

[3].Gounaris E, et al. Zileuton, 5-lipoxygenase inhibitor, acts as a chemopreventive agent in intestinal polyposis, by modulating polyp and systemic inflammation. PLoS One. 2015 Mar 6;10(3):e0121402.