Molecular Weight(MW): 392.49
Ivacaftor (VX-770) is a selective potentiator of CFTR targeting G551D-CFTR and F508del-CFTR with EC50 of 100 nM and 25 nM in fisher rat thyroid cells, respectively.
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(A) CFTR Western blot of normal (NL) and CF HBE cultures treated with VX-809 (5 uM) ± VX-770 (5 uM) for 48 hours. “*” indicates the mature, complex glycosylated form of CFTR, band C; “•” indicates the immature band B. (B) Turnover of rescued ΔF508 in BHK-21 cells. ΔF508 was rescued at 27°C in the presence of VX-809 ± VX-770 for 24 hours. After adding cycloheximide (200 ug/ml, 37°C), cells were lysed at the indicated times and analyzed by Western blotting.
Sci Transl Med 2014 6(246), 246ra96. Ivacaftor (VX-770) purchased from Selleck.
(A) Representative traces of Ca2+ mobilization induced by 100 μm of OAG after modulation of CFTR activity with 10 μm VX-770. (B) Histograms show normalized AUC corresponding to Ca2+ mobilization induced by 100 μm OAG (n, number of cells recorded/N, number of cell passages).
Ivacaftor (VX-770) purchased from Selleck.
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Choose Selective CFTR Inhibitors
|Description||Ivacaftor (VX-770) is a selective potentiator of CFTR targeting G551D-CFTR and F508del-CFTR with EC50 of 100 nM and 25 nM in fisher rat thyroid cells, respectively.|
|Features||The first potent and orally available CFTR potentiator to enter human clinical trials.|
Ivacaftor (10 μM) significantly increases the forskolin-stimulated Cl- secretion (IT) by ~4-fold with an EC50 of 100 nM in the recombinant Fisher rat thyroid (FRT) cells expressing G551D gating mutation of CFTR, and by ~6-fold with an EC50 of 25 nM in the recombinant cells expressing temperature-corrected F508del processing mutation of CFTR. Consistent with the increases in the forskolin-stimulated IT, Ivacaftor (10 μM) increases the open probability (Po) of G551D-, F508del-, and wild-type CFTR by ~6-fold, ~5-fold and ~2-fold, respectively, indicating that Ivacaftor acts directly on CFTR to increase its gating activity. In primary cultured human CF bronchial epithelia (HBE) carrying the G551D and F508del CFTR mutations, Ivacaftor (10 μM) potently increases the forskolin-stimulated IT by ~10-fold from 5% to a maximum level of 48% of that measured in non-CF HBE, with an EC50 of 236 nM displaying ~70-fold more potency compared with the commonly used CFTR potentiator genistein, which has an EC50 of 16 μM. In HBE with F508del homozygous CFTR, Ivacaftor causes a significant increase in the forskolin-stimulated IT with an EC50 of 22 nM, to a less extent from 4% to 16% of non-CF HBE compared with the effect in G551D/F508del HBE. Due to CFTR potentiation, Ivacaftor inhibits excessive ENaC-mediated Na+ and fluid absorption with an IC50 of 43 nM, and decreases the amiloride response, resulting in an increase in the surface fluid and cilia beat frequency (CBF) in G551D/F508del HBE. 
|In vitro||DMSO||78 mg/mL (198.73 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03439865||Not yet recruiting||Chronic Rhinosinusitis (Diagnosis)||University of Alabama at Birmingham|National Heart Lung and Blood Institute (NHLBI)||July 2019||Early Phase 1|
|NCT03251911||Not yet recruiting||Chronic Bronchitis||University of Alabama at Birmingham||January 1 2019||Phase 4|
|NCT03624101||Not yet recruiting||Cystic Fibrosis||University of Alabama at Birmingham||November 1 2018||Early Phase 1|
|NCT02653027||Withdrawn||Diabetes|Cystic Fibrosis||Massachusetts General Hospital||January 1 2018||Not Applicable|
|NCT03277196||Recruiting||Cystic Fibrosis||Vertex Pharmaceuticals Incorporated||August 16 2017||Phase 3|
|NCT03068312||Active not recruiting||Cystic Fibrosis||Vertex Pharmaceuticals Incorporated||July 18 2017||Phase 3|
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