Ivacaftor是CFTR的增强剂,对G551D-CFTR和F508del-CFTR的EC50分别为100 nM和25 nM。
Ivacaftor (VX-770) is a potentiator of CFTR targeting G551D-CFTR and F508del-CFTR with EC50 of 100 nM and 25 nM in fisher rat thyroid cells, respectively.
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。
[1] Van Goor F, et al. Proc Natl Acad Sci U S A, 2009, 106(44), 18825-18830.
[2] Accurso FJ, et al. Effect of VX-770 in persons with cystic fibrosis and the G551D-CFTR mutation. N Engl J Med. 2010 Nov 18;363(21):1991-2003.
分子式 C24H28N2O3 |
分子量 392.49 |
CAS号 873054-44-5 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 78 mg/mL |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02194881 | Cystic Fibrosis | Drug: CF patients with a G551D mutation and treated with Ivacaftor | Assistance Publique - H么pitaux de Paris|Vaincre la Mucoviscidose | 2014-10-01 | 2016-07-31 | |
NCT01784419 | Cystic Fibrosis | Drug: ivacaftor | University of California, San Francisco | 2013-10-01 | 2014-10-17 | |
NCT01705145 | Cystic Fibrosis | Drug: Ivacaftor | Vertex Pharmaceuticals Incorporated|Cystic Fibrosis Foundation Therapeutics | Phase 3 | 2013-01-01 | 2016-03-09 |
NCT03085485 | Chronic Obstructive Pulmonary Disease|Chronic Bronchitis | Drug: Ivacaftor 150 MG|Drug: Placebo | University of Alabama at Birmingham|National Heart, Lung, and Blood Institute (NHLBI)|Vertex Pharmaceuticals Incorporated | Phase 2 | 2017-03-01 | 2017-03-14 |
NCT02310789 | Cystic Fibrosis | Drug: Ivacaftor | Richard Barry Moss|Stanford University | Early Phase 1 | 2015-07-01 | 2016-04-23 |
NCT01614457 | Cystic Fibrosis | Drug: Ivacaftor|Drug: Placebo | Vertex Pharmaceuticals Incorporated|Cystic Fibrosis Foundation Therapeutics | Phase 3 | 2012-07-01 | 2015-01-31 |
NCT01946412 | Cystic Fibrosis | Drug: Ivacaftor | Vertex Pharmaceuticals Incorporated|Cystic Fibrosis Foundation Therapeutics | Phase 3 | 2013-12-01 | 2016-12-06 |
NCT01707290 | Cystic Fibrosis | Drug: ivacaftor | Vertex Pharmaceuticals Incorporated|Cystic Fibrosis Foundation Therapeutics | Phase 3 | 2013-02-01 | 2016-05-10 |
NCT02934698 | Cystic Fibrosis | Drug: Ivacaftor | Medical University of South Carolina|Vertex Pharmaceuticals Incorporated | Phase 3 | 2016-10-01 | 2016-10-14 |
NCT02725567 | Cystic Fibrosis | Drug: ivacaftor | Vertex Pharmaceuticals Incorporated | Phase 3 | 2016-03-01 | 2017-03-22 |
NCT01899105 | Cystic Fibrosis | Drug: lumacaftor|Drug: ivacaftor | Vertex Pharmaceuticals Incorporated | Phase 1 | 2013-07-01 | 2014-04-02 |
NCT02412111 | Cystic Fibrosis | Drug: ivacaftor|Drug: VX-661|Drug: Placebo | Vertex Pharmaceuticals Incorporated | Phase 3 | 2015-06-01 | 2017-02-23 |
NCT02135432 | Chronic Obstructive Pulmonary Disease | Drug: Ivacaftor|Drug: Placebo | University of Alabama at Birmingham | Early Phase 1 | 2015-05-01 | 2017-01-05 |
NCT01897233 | Cystic Fibrosis | Drug: Lumacaftor|Drug: Ivacaftor | Vertex Pharmaceuticals Incorporated | Phase 3 | 2013-07-01 | 2016-10-07 |
NCT01614470 | Cystic Fibrosis | Drug: Ivacaftor|Drug: Placebo | Vertex Pharmaceuticals Incorporated|Cystic Fibrosis Foundation Therapeutics | Phase 3 | 2012-07-01 | 2014-10-23 |
NCT02565914 | Cystic Fibrosis | Drug: VX-661/ivacaftor|Drug: ivacaftor | Vertex Pharmaceuticals Incorporated | Phase 3 | 2015-08-01 | 2016-04-27 |
NCT01685801 | Cystic Fibrosis | Drug: Ivacaftor|Drug: Placebo-matched-to-ivacaftor tablet | Vertex Pharmaceuticals Incorporated | Phase 2 | 2012-09-01 | 2015-04-30 |
NCT00953706 | Cystic Fibrosis | Drug: Ivacaftor|Drug: Placebo | Vertex Pharmaceuticals Incorporated|Cystic Fibrosis Foundation Therapeutics | Phase 2 | 2009-09-01 | 2015-08-27 |
NCT03068312 | Cystic Fibrosis | Drug: Ivacaftor|Drug: Placebo | Vertex Pharmaceuticals Incorporated | Phase 3 | 2017-04-25 | 2017-02-24 |
NCT02742519 | Cystic Fibrosis | Drug: ivacaftor|Drug: Placebo | Vertex Pharmaceuticals Incorporated | Phase 3 | 2016-05-01 | 2016-12-12 |
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。
相关化合物库
使用AMQUAR产品发表文献后请联系我们