Ivacaftor (VX-770)

For research use only.

Catalog No.S1144

131 publications

Ivacaftor (VX-770) Chemical Structure

CAS No. 873054-44-5

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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Selleck's Ivacaftor (VX-770) has been cited by 131 publications

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Biological Activity

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.
F508del-CFTR [1]
(Fisher rat thyroid cells)
G551D-CFTR [1]
(Fisher rat thyroid cells)
25 nM(EC50) 100 nM(EC50)
In vitro

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. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HBE  MX\GeY5kfGmxbjDBd5NigQ>? MlW2NVAh|ryP Mk\GNVAhdWmw Mo\BZZVodWWwdIOgR2ZVWi2mZYDlcoRmdnRiaX;uJJRz[W6|cH;yeOKh Mo\KNlQyODZ6MEG=
CFBE41o- NXrtR2RuTnWwY4Tpc44hSXO|YYm= NFLVe2syOCEEtV2= MWrpcoR2[2W|IILvZpV{fCCrbnPy[YF{\XNiaX6gZY5qd25idILhcpNxd3K2 MVuyNlc3QDF|MB?=
HBE  NGXlcI5HfW6ldHnvckBCe3OjeR?= MVGxNEDDvU1? MnHMZZVodWWwdIOgR2ZVWi2mZYDlcoRmdnRiYX7pc44hfHKjboPwc5J1KGGldHn2bZR6 NF\5dWUzOjd4OEGzNC=>
HBE  MmS5SpVv[3Srb36gRZN{[Xl? NYi1WmF{OTBiwsXN M3qxUlI1KGh? MYXpcoR2[2W|IHGgcY9l\XO2IHL1eEB{cWewaX\pZ4FvfCCrbnPy[YF{\SCrbjDBV2wh\GWydHi= NVHZT5o{OjJ5NkixN|A>
HBE  M4H6cWZ2dmO2aX;uJGF{e2G7 MlLiNVAhyrWP MmnmdI91\W62aXH0[ZMhS0[WUj3k[ZBmdmSnboSgTZNkNCC{ZXfhdoRt\XO|IH;mJJBzcW:{IHHkcYlvcXO2cnH0bY9vKG:oIFPTSS=> MmHFNlI4PjhzM{C=
HBE  NFzJb3BHfW6ldHnvckBCe3OjeR?= MXmxNEDDvU1? NX3wVW9YeGG{dHnhcIx6KHKnc4TvdoV{KGSncHzleIlwdiCxZjDBV2wh\GWydHigbY4hS1OHIITy[YF1\WRibX;uc4xigWW{cx?= MYGyNlc3QDF|MB?=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
PPARγ / pERK; 

PubMed: 30498130     

Caco-2 cells incubated with P31–43 in the presence or absence of VX-770. Immunoblot of PPARc or phospho-ERK1/2 (phERK1/2) and densitometric analysis of protein levels relative to b-actin.


PubMed: 30498130     

Immunoblotting with specific antibodies (NLRP3) in Caco-2 cells challenged for 2 or 4 h in the presence or absence of VX-770. NLRP3 expression.


PubMed: 25101887     

Effect of VX-770 on the expression pattern of low temperature-rescued ΔF508-CFTR-3HA determined by immunoblot. Cells were treated with VX-770 alone for 24 hours at 26°C. CFTR was visualized with anti-HA antibody, and anti–Na+/K+-ATPase antibody served as loading control. 

30498130 25101887

PubMed: 30498130     

Confocal image staining with anti-F-actin. DAPI (blue), nuclear counterstaining. Scale bar, 50 μm.



Solubility (25°C)

In vitro DMSO 78 mg/mL (198.73 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 392.49


CAS No. 873054-44-5
Storage powder
in solvent
Synonyms N/A
Smiles CC(C)(C)C1=CC(=C(C=C1NC(=O)C2=CNC3=CC=CC=C3C2=O)O)C(C)(C)C

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04254705 Not yet recruiting Procedure: Rectal Biopsy Cystic Fibrosis Universitaire Ziekenhuizen Leuven|Vertex Pharmaceuticals Incorporated|KU Leuven|University of Lisbon March 1 2020 Not Applicable
NCT03085485 Recruiting Drug: Ivacaftor 150 MG|Drug: Placebo Chronic Obstructive Pulmonary Disease|Chronic Bronchitis University of Alabama at Birmingham|National Heart Lung and Blood Institute (NHLBI)|Vertex Pharmaceuticals Incorporated March 16 2017 Phase 2
NCT02724527 Unknown status Drug: Cavosonstat|Drug: Placebo Cystic Fibrosis Nivalis Therapeutics Inc. April 2016 Phase 2
NCT02725567 Recruiting Drug: ivacaftor Cystic Fibrosis Vertex Pharmaceuticals Incorporated March 2016 Phase 3

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CFTR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID