|1-(1-(苯并[b]噻吩-2-基)乙基)-1-羟基脲|CsnPharm

CAS No.: 111406-87-2

Zileuton/齐留通 Catalog No. CSN12237

Synonyms: A 64077;Abbott 64077;trade name ZYFLO

Zileuton is a reversible 5-lipoxygenase inhibitor with IC50 value of 0.5 µM in rat basophilic leukemia-1 (RBL-1) cells. It also potently inhibited leukotriene B4 production with an IC50 value of 0.6 µM in purified human peripheral blood polymorphonuclear leukocytes (PMNL).

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技术信息

生物活性

描述Leukotrienes (LT) are metabolites of arachidonic acid (AA) formed from the 5-lipoxygenase (5-LOX) pathway. They exhibit a number of biological effects such as contraction of smooth muscles, especially bronchoconstriction, increased vascular permeability, and migration of leukocytes to areas of inflammation. Zileuton is a potent and selective inhibitor of 5-lipoxygenase with antiasthmatic properties^[3]. In macrophages, zileuton overinterfered with arachidonic acid (AA) release to inhibit PG biosynthesis. In activated mouse peritoneal macrophages and macrophage J774, zileuton significantly reduces PGE2 and 6-ketone prostaglandin F1α (PGF1α) levels^[4]. In anti-CD3-treated cells, IL-2 decreased in zileuton-treated and untreated cells with increasing incubation time. Zileuton likely reduced IL-2 levels by inhibiting 5-lipoxygenase^[3]. Zileuton treatement on rats with TNB colitis, however, showed a significant reduction in the macroscopic damage score after four weeks of treatment compared with 5-ASA and placebo groups. The intracolonic administration of 50 mg/kg of zileuton after colitis induction decreased the local peak release of LTB₄ by 90%^[5]. In zileuton (5 mg/kg, p.o.) treated ischemia/reperfusion (I/R) rat, the effect of zileuton to decrease NF-κB expression did not change significantly in the presence of COX inhibitors, and the group revealed significantly lower level of NF-κB staining. Zileuton (5 mg/kg, p.o.) treatment given to I/R rats decreased apoptotic index significantly. In 5-LOX gene knockout mice, administration of zileuton before I/R significantly reduced the degree of renal dysfunction (urea, creatinine) and injury (AST, histology). In addition, zileuton reduced the expression of ICAM-1 and the associated polymorphonuclear leukocyte infiltration caused by I/R of the mouse kidney^[6]. Although zileuton inhibited LTB₄ production in the peritonitis model more effectively than the LTA₄H inhibitor, the influx of neutrophils into the peritoneum after 1 and 2h was significantly higher in zileuton- versus JNJ-26993135-treated animals^[7].
动物研究
剂量
Mice: 10 mg/kg^[3] (i.p.); 50 mg/kg^[4] (p.o.) Rat: 1 mg/kg, 3 mg/kg^[5] (i.v.)

给药途径
i.p., i.v., p.o.
临床研究

动物研究
剂量	Mice: 10 mg/kg^[3] (i.p.); 50 mg/kg^[4] (p.o.) Rat: 1 mg/kg, 3 mg/kg^[5] (i.v.)
给药途径	i.p., i.v., p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00595114	-	-	Completed	-	United States, Massachusetts ... more >> Brigham and Women's Hospital Boston, Massachusetts, United States, 02115 Collapse <<
NCT00595114	-	-	Completed	-	-
NCT01125748	-	-	Completed	-	-

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.2321 mL
- 21.1604 mL
- 42.3208 mL
- 5 mM
- 0.8464 mL
- 4.2321 mL
- 8.4642 mL
- 10 mM
- 0.4232 mL
- 2.1160 mL
- 4.2321 mL

技术信息

CAS号

111406-87-2

储存条件

粉末: Keep in dark place,Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C11H12N2O2S

运输

蓝冰

分子量

236.29

别名

A 64077;Abbott 64077;trade name ZYFLO;ZYFLO CR;齐留通

溶解度

DMSO	50.0 mg/mL (211.6 mM)
Water	insoluble

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT00595114	-	-	Completed	-	United States, Massachusetts ... more >> Brigham and Women's Hospital Boston, Massachusetts, United States, 02115 Collapse <<
NCT00595114	-	-	Completed	-	-
NCT01125748	-	-	Completed	-	-
NCT00467831	Hermansky-Pudlak Syndrome (HPS... more >>) Pulmonary Fibrosis Oculocutaneous Albinism Platelet Storage Pool Deficiency Metabolic Disease Collapse <<	Phase 1 Phase 2	Terminated(insufficient enroll... more >>ment) Collapse <<	-	United States, Maryland ... more >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 Collapse <<
NCT01125748	Allergic Asthma	Phase 4	Completed	-	-
NCT00467831	-	-	Terminated(insufficient enroll... more >>ment) Collapse <<	-	-
NCT00723021	-	-	Completed	-	-
NCT01805687	Asthma	Phase 4	Completed	-	United States, Massachusetts ... more >> Northeast Medical Research Associates North Dartmouth, Massachusetts, United States, 02747 Collapse <<
NCT00723021	Asthma	Phase 2	Completed	-	United States, Maryland ... more >> Pfizer Investigational Site Baltimore, Maryland, United States, 21225 United States, Massachusetts Pfizer Investigational Site North Dartmouth, Massachusetts, United States, 02747 United States, Michigan Pfizer Investigational Site Kalamazoo, Michigan, United States, 49007 United States, Nebraska Pfizer Investigational Site Omaha, Nebraska, United States, 68131 Collapse <<
NCT00070486	Lung Cancer	Phase 2	Completed	-	-
NCT01174056	Lung Inflammation	Early Phase 1	Completed	-	United States, Missouri ... more >> Washington University / Barnes Jewish Hospital St. Louis, Missouri, United States, 63110 Collapse <<
NCT01805687	-	-	Completed	-	-
NCT00299065	Asthma	Phase 1 Phase 2	Completed	-	United States, California ... more >> Allergy & Asthma Specialist Medical Group Huntington Beach, California, United States, 92647 Allergy and Asthma Medical Group and Research Center San Diego, California, United States, 92123 United States, Colorado Colorado Allergy and Asthma Centers, PC Englewood, Colorado, United States, 80112 United States, Massachusetts Northeast Medical Research Associates North Dartmouth, Massachusetts, United States, 02747 United States, Minnesota Clinical Research Institute Minneapolis, Minnesota, United States, 55402 United States, Missouri The Clinical Research Center, L.L.C. St. Louis, Missouri, United States, 63141 United States, New Jersey Princeton Center for Clinical Research Skillman, New Jersey, United States, 08558 United States, Ohio Bernstein Clinical Research Center Cincinnati, Ohio, United States, 45231 United States, Oregon Allergy Associates Research Center Portland, Oregon, United States, 97213 United States, Texas Western Sky Medical Research El Paso, Texas, United States, 79902 Collapse <<
NCT00056004	Head and Neck Cancer ... more >> Lung Cancer Collapse <<	Phase 2	Completed	-	United States, Michigan ... more >> Barbara Ann Karmanos Cancer Institute Detroit, Michigan, United States, 48201-1379 Collapse <<
NCT00493974	Pulmonary Disease, Chronic Obs... more >>tructive Collapse <<	Phase 3	Terminated(Lack of feasibility... more >> due to low recruitment) Collapse <<	-	United States, Alabama ... more >> University of Alabama Lung Health Center Birmingham, Alabama, United States, 35249 Veteran's Administration Medical Center Birmingham, Alabama, United States, 35294 United States, California LA BioMed at Harbor, University of California Los Angeles, California, United States, 90502 University of California San Francisco-Airway Clinical Research Center San Francisco, California, United States, 94143 United States, Colorado Denver Health Medical Center Denver, Colorado, United States, 80204 National Jewish Medical and Research Center Denver, Colorado, United States, 80206 Veteran's Administration Medical Center Denver, Colorado, United States, 80220 United States, Maryland University of Maryland Hospital Baltimore, Maryland, United States, 21201 United States, Massachusetts Fallon Clinic Boston, Massachusetts, United States, 01605 Brigham and Women's Hospital Boston, Massachusetts, United States, 02115 Veteran's Administration Medical Center Boston, Massachusetts, United States, 02132 United States, Michigan Veteran's Administration Medical Center Ann Arbor, Michigan, United States, 48105 University of Michigan Medical Center Ann Arbor, Michigan, United States, 48109 United States, Minnesota Veteran's Administration Medical Center Minneapolis, Minnesota, United States, 55417 HealthPartners Research Foundation Minneapolis, Minnesota, United States, 55440 Mayo Clinic Rochester, Minnesota, United States, 55905 United States, Pennsylvania Temple University Lung Center Philadelphia, Pennsylvania, United States, 19140 University of Pittsburgh Emphysema Research Center Pittsburgh, Pennsylvania, United States, 15213 Collapse <<
NCT00262405	Idiopathic Pulmonary Fibrosis	Phase 2	Completed	-	United States, Michigan ... more >> University of Michigan Ann Arbor, Michigan, United States, 48109 Collapse <<
NCT00493974	-	-	Terminated(Lack of feasibility... more >> due to low recruitment) Collapse <<	-	-
NCT01021215	-	-	Completed	-	-
NCT00486343	Asthma	Phase 4	Terminated(Slower than anticip... more >>ated enrollment) Collapse <<	June 2008	United States, Massachusetts ... more >> Critical Therapeutics Lexington, Massachusetts, United States, 02421 Collapse <<
NCT00575861	Asthma	Phase 4	Completed	-	United States, California ... more >> Arthur F Gelb Medical Corporation Lakewood, California, United States, 90712 Collapse <<
NCT00098358	Acne Vulgaris	Phase 2	Unknown	-	United States, California ... more >> Therapeutics Clinical Research San Diego, California, United States, 92123 United States, Georgia MedaPhase, Inc. Newnan, Georgia, United States, 30263 United States, Kentucky Dermatology Specialists, PSC Louisville, Kentucky, United States, 40202 United States, Minnesota Minnesota Clinical Study Center Fridley, Minnesota, United States, 55432 United States, New Mexico Academic Dermatology Associates Albuquerque, New Mexico, United States, 87106 United States, New York SUNY Downstate Medical Center Brooklyn, New York, United States, 11203 Dermatology Associates of Rochester Rochester, New York, United States, 14623 United States, Pennsylvania Milton S. Hersey Medical Center Hersey, Pennsylvania, United States, 17033-0850 United States, Tennessee Rivergate Dermatology Goodlettsville, Tennessee, United States, 37072 United States, Texas DermResearch, Inc. Austin, Texas, United States, 78759 J&S Studies, Inc. Bryan, Texas, United States, 77802 United States, Virginia Virginia Clinical Research, Inc. Norfolk, Virginia, United States, 23507 Collapse <<
NCT00534625	Asthma	Phase 2	Completed	-	-
NCT01136941	Sickle Cell Disease	Phase 1	Completed	-	United States, Ohio ... more >> Cincinnati Children's Hospital Medical Center Cincinnati, Ohio, United States, 45229 Collapse <<
NCT01021215	Tobacco Use Disorder	Phase 1 Phase 2	Completed	-	United States, New York ... more >> Weill Cornell Medical College in New York City, Cornell University New York, New York, United States, 10021 United States, Texas MD Anderson Cancer Center - Consortium Lead Organzation Houston, Texas, United States, 77030 Collapse <<
NCT01130688	Chronic Myelogenous Leukemia	Phase 1	Terminated(Lack of enrollment)	-	United States, Massachusetts ... more >> University of Massachusetts Medical School Worcester, Massachusetts, United States, 01655 Collapse <<
NCT02047149	Chronic Myelogenous Leukemia	Phase 1	Terminated(Low accrual)	-	United States, Massachusetts ... more >> University of Massachusetts Medical School Worcester, Massachusetts, United States, 01655 Collapse <<
NCT02348203	Current Every Day Smoker ... more >> Multiple Pulmonary Nodules Tobacco Smoking Tobacco Use Disorder Collapse <<	Phase 2	Recruiting	-	United States, Arizona ... more >> The University of Arizona Medical Center-University Campus Recruiting Tucson, Arizona, United States, 85724 Contact: Linda L. Garland 520-626-3434 lgarland@azcc.arizona.edu Principal Investigator: Linda L. Garland United States, California University of California Davis Comprehensive Cancer Center Recruiting Sacramento, California, United States, 95817 Contact: Jun Yan 530-752-5109 junyang@ucdavis.edu Principal Investigator: Jun Yan United States, Massachusetts Boston University School of Medicine Recruiting Boston, Massachusetts, United States, 02118 Contact: Avrum Spira 617-414-6960 aspira@bu.edu Principal Investigator: Avrum Spira Collapse <<

Zileuton/齐留通 Catalog No. CSN12237

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