Ivacaftor (VX-770)

Catalog No.S1144

Ivacaftor (VX-770) Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 112 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
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7 Customer Reviews

  • (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.

    Treatment with DF508 CFTR correcting drugs (VX-770 and VX-809, 10 lM) partially redistributed F-actin in the submembrane compartment as also shown by the two small membrane peaks in the quantification graph. Treatment with PP2 (1 lM) alone or in combination with VX-770 and VX-809 completely recovered the actin distribution in DF508-chol similar to Control-chol. Phalloidin fluorescence intensity confirms the presence of membrane sharper peaks that reach intensity values comparable to Control-chol. Abbreviations: A.U, arbitrary units; chol, cholangiocytes.

    Hepatology, 2018, 67(3):972-988. Ivacaftor (VX-770) purchased from Selleck.

  • (A, B) Liquid absorption (Jv) was assessed in expanded alveolar epithelial cells from WT pigs under basal conditions (A) or following treatment with forskolin+IBMX (5+50 μmol/L, B) in the absence or presence of 10 μmol/L ivacaftor. n=10 transwells from 3 pigs.

    Crit Care Med, 2017, 45(12):e1240-e1246. Ivacaftor (VX-770) purchased from Selleck.

    All curves in the presence of 50 μMforskolin. (A) VX-770, EC50 = 441 nM± 144, nH = 0.82 ± 0.2, n = 3 wells from one experiment.

    Br J Pharmacol, 2017, 174(7):525-539. Ivacaftor (VX-770) purchased from Selleck.

  • Mol Pharmacol, 2018, doi: 10.1124/mol.118.112177. 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.


    (C) Representative traces of iodide efflux curves after CFTR stimulation with 10 μm VX-770 or 100μm OAG. (D) Histograms show the mean relative rate of CFTR activity for the experimental condition indicated below each bar (n = 4).

    Ivacaftor (VX-770) purchased from Selleck.

Purity & Quality Control

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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  NIrEfWdHfW6ldHnvckBCe3OjeR?= MXSxNEDPxE1? MUKxNEBucW5? MoHiZZVodWWwdIOgR2ZVWi2mZYDlcoRmdnRiaX;uJJRz[W6|cH;yeOKh M1nNVFI1OTB4OECx
CFBE41o- NUm0emVGTnWwY4Tpc44hSXO|YYm= NXi3TYQ5OTBiwsXN MoDlbY5lfWOnczDyc4J2e3RiaX7jdoVie2W|IHnuJIFvcW:wIITyZY5{eG:{dB?= NES3dZIzOjd4OEGzNC=>
HBE  MoLjSpVv[3Srb36gRZN{[Xl? NXHLTZhvOTBiwsXN M2\6PYF2\22nboTzJGNHXFJvZHXw[Y5l\W62IHHubY9vKHS{YX7zdI9zfCCjY4Tpeol1gQ>? NV[2VFJSOjJ5NkixN|A>
HBE  MX7GeY5kfGmxbjDBd5NigQ>? NXnNOYx4OTBiwsXN M{fRdlI1KGh? MlzJbY5lfWOnczDhJI1w\GW|dDDieZQhe2mpbnnmbYNidnRiaX7jdoVie2ViaX6gRXNNKGSncITo MnzsNlI4PjhzM{C=
HBE  NVG0ZWRsTnWwY4Tpc44hSXO|YYm= MUSxNEDDvU1? M3zGZZBwfGWwdHnheIV{KEOIVGKt[IVx\W6mZX70JGl{[yxicnXnZZJldGW|czDv[kBxemmxcjDh[I1qdmm|dILheIlwdiCxZjDDV2U> MmDhNlI4PjhzM{C=
HBE  NUX2TYRpTnWwY4Tpc44hSXO|YYm= NEnjU3IyOCEEtV2= MmC4dIFzfGmjbHz5JJJme3SxcnXzJIRmeGyndHnvckBw\iCDU1yg[IVxfGhiaX6gR3NGKHS{ZXH0[YQhdW:wb3zhfYVzew>? MlX3NlI4PjhzM{C=

... Click to View More Cell Line Experimental Data


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

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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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CFTR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID