Home > Phosphodiesterase (PDE) & > Roflumilast

Roflumilast

罗氟司特,APTA 2217,B9302-107,BY 217,BYK 20869,APTA-2217,APTA2217,BYK20869

Roflumilast 是一种选择性的PDE-4抑制剂，IC50为0.2-4.3 nM。

目录号
EY1322
EY1322
EY1322
EY1322
纯度
99.41%
99.41%
99.41%
99.41%
规格
1 mg
5 mg
10 mg
50 mg
原价
220
530
616
2760
售价
220
530
616
2760
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
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  • 生物活性

    Roflumilast is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM in a cell-free assay.

  • 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 A的Km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] Hatzelmann A, et al. Pulm Pharmacol Ther, 2010, 23(4), 235-256.

    分子式
    C17H14Cl2F2N2O3    		 分子量
    403.21    		 CAS号
    162401-32-3    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    80 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    15 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
    NCT01354782 Chronic Obstructive Pulmonary Disease Drug: Roflumilast AstraZeneca Phase 1 2011-05-01 2016-10-24
    NCT02018432 Chronic Obstructive Pulmonary Disease Drug: Roflumilast escalation dosage|Drug: Roflumilast conventional dosage Asan Medical Center Phase 4 2013-12-01 2013-12-17
    NCT01830959 Sarcoidosis Drug: Roflumilast|Drug: Placebo University of Cincinnati|The Cleveland Clinic|University of Pittsburgh|University of Illinois at Chicago|Henry Ford Health System|Albany Medical College Phase 4 2013-04-01 2015-12-04
    NCT02068456 Chronic Obstructive Pulmonary Disease Drug: Roflumilast AstraZeneca 2012-09-01 2016-12-01
    NCT02097992 COPD Drug: roflumilast|Drug: placebo|Drug: roflumilast 500g single dose|Drug: placebo single dose University of Miami|Forest Laboratories 2013-02-01 2015-10-22
    NCT01630200 Chronic Obstructive Pulmonary Disease and Allied Conditions Drug: Roflumilast|Drug: Placebo LudwLudwig Boltzmann Institute for COPD and Respiratory Epidemiology|Medical University of Vienna Phase 2 2012-05-01 2015-09-21
    NCT01443845 COPD|COPD Exacerbation|Lung Diseases|Respiratory Disorders|Pulmonary Disease|Chronic Obstructive Lung Diseases|Chronic Obstructive Airway Disease Drug: Roflumilast|Drug: Placebo Forest Laboratories Phase 4 2011-09-01 2016-11-30
    NCT01365533 Allergic Asthma Drug: Roflumilast|Drug: Placebo AstraZeneca Phase 2 2004-12-01 2016-10-24
    NCT02165826 Chronic Obstructive Pulmonary Disease (COPD) Drug: Roflumilast|Drug: Roflumilast Placebo|Drug: Standard of Care COPD Treatment Takeda Phase 3 2014-04-01 2017-01-24
    NCT01765192 Asthma Drug: Roflumilast|Drug: Roflumilast placebo|Drug: Montelukast AstraZeneca Phase 2 2013-02-01 2016-12-02
    NCT01849341 Chronic Obstructive Pulmonary Disease (COPD) Drug: Roflumilast alternated days|Drug: Roflumilast 500 mcg per day Fundacin Pblica Andaluza Progreso y Salud|Andalusian Initiative for Advanced Therapies - Fundacin Pblica Andaluza Progreso y Salud Phase 4 2012-07-01 2015-07-07
    NCT02037672 PCOS|Obesity Drug: metformin|Drug: metformin and roflumilast University Medical Centre Ljubljana Phase 4 2013-09-01 2014-01-21
    NCT02451540 Pulmonary Disease, Chronic Obstructive Radiation: HRCT scan|Drug: Placebo of Roflumilast|Drug: Roflumilast FLUIDDA nv Phase 2 2015-09-01 2017-03-07
    NCT00424268 Chronic Obstructive Pulmonary Disease Drug: Roflumilast|Drug: Placebo AstraZeneca Phase 3 2007-01-01 2016-10-24
    NCT02079844 Schizophrenia Drug: Roflumilast|Drug: Placebo|Drug: Second generation antipsychotic Takeda Phase 1 2014-03-01 2016-08-09
    NCT01572948 COPD Drug: roflumilast|Drug: placebo University of Alabama at Birmingham 2012-06-01 2015-09-28
    NCT01745848 Chronic Obstructive Pulmonary Disease Drug: Roflumilast University of Pittsburgh Phase 4 2013-02-01 2016-09-26
    NCT01701934 Chronic Obstructive Pulmonary Disease|Metabolic Syndrome Drug: Roflumilast|Drug: Placebo Laval University|Innovair|Takeda Phase 2 2013-02-01 2014-11-10
    NCT03073798 COPD|Chronic Bronchitis|Emphysema Drug: Roflumilast|Drug: Placebo Johns Hopkins University Phase 4 2013-03-18 2017-03-02
    NCT01888952 Advanced B-cell Lymphoid Malignancies Drug: Prednisone|Drug: Roflumilast Anand B. Karnad|The University of Texas Health Science Center at San Antonio Early Phase 1 2013-07-01 2017-01-05
    NCT00746382 Dermatitis Drug: Roflumilast cream|Drug: Placebo cream AstraZeneca|Fougera Pharmaceuticals Inc. Phase 2 2008-11-01 2016-11-30
    NCT01973998 COPD Drug: Roflumilast|Drug: Placebo Temple University|Forest Laboratories Phase 3 2013-11-01 2016-10-17
    NCT00313209 Chronic Obstructive Pulmonary Disease (COPD) Drug: Roflumilast|Drug: Placebo AstraZeneca Phase 3 2006-04-01 2016-11-01
    NCT01856764 Atopic Dermatitis Drug: 0.5% Roflumilast Cream|Drug: Vehicle Cream AstraZeneca Phase 2 2013-06-01 2016-12-02
    NCT01595750 Chronic Obstructive Pulmonary Disease Drug: Roflumilast 500|Drug: Placebo Spanish Research Center for Respiratory Diseases Phase 4 2012-05-01 2012-05-09

    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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