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VX-809

VRT 826809,Lumacaftor,VX 809,VX809,VRT826809,VRT-826809,VRT 826809

VX-809能增加突变型CFTR(F508del-CFTR)的成熟,并纠正常见于囊性纤维化的CFTR突变,EC50为0.1 μM。

目录号
EY1047
EY1047
EY1047
EY1047
纯度
99.63%
99.63%
99.63%
99.63%
规格
1 mg
5 mg
10 mg
50 mg
原价
320
740
1020
1600
售价
320
740
1020
1600
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

    VX-809 (Lumacaftor) acts to correct CFTR mutations common in cystic fibrosis by increasing mutant CFTR (F508del-CFTR) maturation,EC50 of 0.1 μM in fisher rat thyroid cells. Phase 3.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    ~0.1 mM

  • 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] Van Goor F, et al. Proc Natl Acad Sci U S A, 2011, 108(46), 18843-18848.

    分子式
    C24H18F2N2O5
    分子量
    452.41
    CAS号
    936727-05-8
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    90 mg/mL
    Water
    <1 mg/mL
    Ethanol
    5 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
    NCT00865904 Cystic Fibrosis Drug: VX-809|Drug: Placebo Vertex Pharmaceuticals Incorporated Phase 2 2009-03-01 2015-08-01
    NCT01216046 Cystic Fibrosis Drug: VX-809|Drug: VX-770|Drug: VX-809 placebo|Drug: VX-770 placebo Vertex Pharmaceuticals Incorporated Phase 1 2010-10-01 2012-01-16
    NCT00966602 Cystic Fibrosis Drug: VX-809|Drug: VX-770|Drug: VX-809 & VX-770|Drug: Placebo Vertex Pharmaceuticals Incorporated Phase 1 2009-09-01 2010-01-02
    NCT01225211 Cystic Fibrosis Drug: Lumacaftor|Drug: Ivacaftor|Drug: Lumacaftor Placebo|Drug: Ivacaftor Placebo Vertex Pharmaceuticals Incorporated Phase 2 2010-10-01 2015-09-02
    NCT01899105 Cystic Fibrosis Drug: lumacaftor|Drug: ivacaftor Vertex Pharmaceuticals Incorporated Phase 1 2013-07-01 2014-04-02
    NCT01897233 Cystic Fibrosis Drug: Lumacaftor|Drug: Ivacaftor Vertex Pharmaceuticals Incorporated Phase 3 2013-07-01 2016-10-07
    NCT02807415 Cystic Fibrosis Drug: Lumacaftor plus Ivacaftor Hannover Medical School|Heidelberg University|University of Giessen 2016-06-01 2016-06-22
    NCT01768663 Cystic Fibrosis Drug: Lumacaftor|Drug: Ivacaftor|Drug: Ciprofloxacin|Drug: Itraconazole|Drug: Rifampin Vertex Pharmaceuticals Incorporated Phase 1 2013-01-01 2013-11-14
    NCT02390219 Cystic Fibrosis|Advanced Lung Disease Drug: Lumacaftor|Drug: Ivacaftor Vertex Pharmaceuticals Incorporated Phase 3 2015-03-01 2016-10-26
    NCT01931839 Cystic Fibrosis, Homozygous or Heterozygous for the F508del-CFTR Mutation Drug: Lumacaftor|Drug: Ivacaftor Vertex Pharmaceuticals Incorporated Phase 3 2013-10-01 2016-04-27
    NCT02514473 Cystic Fibrosis Drug: VX-809|Drug: Placebo|Drug: VX-770 Vertex Pharmaceuticals Incorporated Phase 3 2015-07-01 2016-10-24
    NCT01807923 Cystic Fibrosis, Homozygous for the F508del CFTR Mutation Drug: Lumacaftor Plus Ivacaftor Combination|Drug: Ivacaftor|Drug: Placebo Vertex Pharmaceuticals Incorporated Phase 3 2013-05-01 2015-08-01
    NCT01807949 Cystic Fibrosis, Homozygous for the F508del CFTR Mutation Drug: Placebo|Drug: Lumacaftor Plus Ivacaftor Combination|Drug: Ivacaftor Vertex Pharmaceuticals Incorporated Phase 3 2013-04-01 2016-08-15
    NCT01910415 Cystic Fibrosis Drug: Lumacaftor|Drug: Lumacaftor Placebo|Drug: Ivacaftor|Drug: Ivacaftor Placebo|Drug: moxifloxacin hydrochloride Vertex Pharmaceuticals Incorporated Phase 1 2013-06-01 2014-08-08
    NCT02653027 Diabetes|Cystic Fibrosis Drug: Lumacaftor-ivacaftor|Other: OGTT Massachusetts General Hospital 2016-01-01 2016-01-08
    NCT02858843 Cystic Fibrosis|Diabetes Drug: lumacaftor-ivacaftor Massachusetts General Hospital 2016-08-01 2016-08-15
    NCT02544451 Cystic Fibrosis Drug: Ivacaftor|Drug: Lumacaftor Vertex Pharmaceuticals Incorporated Phase 3 2015-08-01 2016-12-19
    NCT02797132 Cystic Fibrosis Drug: lumacaftor/ ivacaftor Vertex Pharmaceuticals Incorporated Phase 3 2016-05-01 2016-07-22
    NCT01888393 Hepatic Impairment|Healthy Drug: lumacaftor 200 mg q12h + ivacaftor 250 mg q12h Vertex Pharmaceuticals Incorporated Phase 1 2013-06-01 2013-11-18
    NCT02823470 Cystic Fibrosis Drug: LUM/IVA|Device: activated smart device|Device: de-activated smart device Vertex Pharmaceuticals Incorporated Phase 4 2016-06-01 2017-03-22

    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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