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Zileuton

齐留通,A-64077,Zyflo A64077,Abbott 64077,Griluto-CR,Leutrol

Zileuton是一种口服有效的5-脂氧合酶抑制剂,因而可抑制白三烯(LTB 4,LTC 4,LTD 4和LTE 4)的形成。

目录号
EY0887
EY0887
EY0887
EY0887
纯度
99.68%
99.68%
99.68%
99.68%
规格
1 mg
5 mg
10 mg
50 mg
原价
115
232
386
1100
售价
115
232
386
1100
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    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.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 AKm系数


    例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。


  • 参考文献

    [1] Rossi A1, et al. Br J Pharmacol, 2010, 161(3), 555-570.
    [2] McMillan et al (1992) Pre-clinical pharmacology of ICI D2138, a potent orally-active non-redox inhibitor of 5-lipoxygenase. Br.J.Pharmacol. 107 1042.
    [3] Malo et al (1994) The 5-lipoxygenase inhibitory activity of zileuton in in vitro and in vivo models of antigen-induced airway anaphylaxis. Pulm.Pharmacol. 7 73.
    [4] Lu et al (2003) Mechanism-based inhibition of human liver microsomal cytochrome P450 1A2 by zileuton, a 5-lipoxygenase inhibitor. Drug Metab.Dispos. 31 1352.

    分子式
    C11H12N2O2S
    分子量
    236.29
    CAS号
    111406-87-2
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    47 mg/mL
    Water
    <1 mg/mL
    Ethanol
    47 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT01136941 Sickle Cell Disease Drug: Zileuton Children's Hospital Medical Center, Cincinnati Phase 1 2010-09-01 2014-06-17
    NCT01130688 Chronic Myelogenous Leukemia Drug: Zileuton University of Massachusetts, Worcester Phase 1 2010-01-01 2015-05-26
    NCT02047149 Chronic Myelogenous Leukemia Drug: Zileuton (Zyflo庐) Dasatinib (Sprycel庐)|Drug: Dosing with Zileuton/Dasatinib in CML|Drug: Daily dosing of Zileuton/Dasatinib|Drug: Daily dosing with Zileuton/Dasatinib for CML University of Massachusetts, Worcester|Bristol-Myers Squibb Phase 1 2014-01-01 2016-09-29
    NCT00575861 Asthma Drug: zileuton Gelb, Arthur F., M.D. Phase 4 2005-09-01 2007-12-18
    NCT00486343 Asthma Drug: Zileuton CR|Drug: Placebo Critical Therapeutics Phase 4 2007-07-01 2008-04-01
    NCT02348203 Pulmonary Nodules|Tobacco Use Disorder Drug: Aspirin|Other: Laboratory Biomarker Analysis|Other: Placebo|Other: Placebo|Drug: Zileuton National Cancer Institute (NCI) Phase 2 2016-01-01 2017-01-31
    NCT00262405 Idiopathic Pulmonary Fibrosis Drug: zileuton|Drug: azathioprine/prednisone University of Michigan|National Institutes of Health (NIH) Phase 2 2001-01-01 2015-12-02
    NCT00534625 Asthma Drug: zileuton|Drug: placebo|Drug: zileuton Critical Therapeutics Phase 2 2007-09-01 2008-03-19
    NCT00493974 Pulmonary Disease, Chronic Obstructive Drug: Zileuton|Drug: Placebo University of Minnesota - Clinical and Translational Science Institute|National Heart, Lung, and Blood Institute (NHLBI) Phase 3 2007-03-01 2016-08-24
    NCT00056004 Head and Neck Cancer|Lung Cancer Drug: zileuton Barbara Ann Karmanos Cancer Institute|National Cancer Institute (NCI) Phase 2 2003-06-01 2013-04-25
    NCT01021215 Tobacco Use Disorder Drug: Zileuton|Drug: Celecoxib|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 1|Phase 2 2010-05-01 2015-04-01
    NCT00098358 Acne Vulgaris Drug: Zileuton Critical Therapeutics Phase 2 2004-11-01 2007-02-05
    NCT00299065 Asthma Drug: Zileuton injection Critical Therapeutics Phase 1|Phase 2 2006-01-01 2007-09-24
    NCT01805687 Asthma Drug: Zileuton extended release Cornerstone Therapeutics Inc. Phase 4 2013-03-01 2014-08-22
    NCT00070486 Lung Cancer Drug: carboplatin|Drug: celecoxib|Drug: gemcitabine hydrochloride|Drug: zileuton Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) Phase 2 2003-12-01 2016-06-28
    NCT01174056 Lung Inflammation Drug: Zileuton|Drug: Pioglitazone placebo|Drug: Zileuton placebo|Drug: Pioglitazone Washington University School of Medicine|Doris Duke Charitable Foundation Early Phase 1 2011-07-01 2014-04-22
    NCT00467831 Hermansky-Pudlak Syndrome (HPS)|Pulmonary Fibrosis|Oculocutaneous Albinism|Platelet Storage Pool Deficiency|Metabolic Disease Drug: Losartan|Drug: Zileuton|Drug: N-Acetylcysteine|Drug: Pravastatin|Drug: Erythromycin National Human Genome Research Institute (NHGRI)|National Institutes of Health Clinical Center (CC) Phase 1|Phase 2 2007-04-01 2013-06-03
    NCT00723021 Asthma Drug: PF-04191834|Drug: PF-04191834|Drug: PF-04191834|Drug: zileuton|Drug: Placebo Pfizer Phase 2 2008-07-01 2012-12-27
    NCT01125748 Allergic Asthma Drug: Omalizumab|Drug: Placebo|Drug: Asthma therapies Genentech, Inc. Phase 4 2010-05-01 2014-10-08
    NCT00595114 Asthma|Pulmonary Disease, Chronic Obstructive Brigham and Women's Hospital|National Heart, Lung, and Blood Institute (NHLBI) Early Phase 1 2007-12-01 2016-09-04

    注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。

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