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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3 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.

     

    (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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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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.
Targets
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  M4jkc2Z2dmO2aX;uJGF{e2G7 MWixNEDPxE1? MlvlNVAhdWmw MV7heYdu\W62czDDSnRTNWSncHXu[IVvfCCrb36geJJidnOyb4L0xsA> NIPwfVAzPDFyNkiwNS=>
CFBE41o- NIHLd3pHfW6ldHnvckBCe3OjeR?= NED2[JUyOCEEtV2= NVrKU2JLcW6mdXPld{Bzd2K3c4SgbY5kemWjc3XzJIlvKGGwaX;uJJRz[W6|cH;yeC=> M2jsTlIzPzZ6MUOw
HBE  NYHDV|h{TnWwY4Tpc44hSXO|YYm= MXSxNEDDvU1? NX\4TWpl[XWpbXXueJMhS0[WUj3k[ZBmdmSnboSgZY5qd25idILhcpNxd3K2IHHjeIl3cXS7 MYCyNlc3QDF|MB?=
HBE  NH7J[FhHfW6ldHnvckBCe3OjeR?= MnTQNVAhyrWP MkXyNlQhcA>? NF6xfWpqdmS3Y3XzJIEhdW:mZYP0JIJ2fCC|aXfubYZq[2GwdDDpcoNz\WG|ZTDpckBCW0xiZHXweIg> NHy0d5EzOjd4OEGzNC=>
HBE  NGr2Z|RHfW6ldHnvckBCe3OjeR?= M4LvblExKML3TR?= MYjwc5RmdnSrYYTld{BETlSULXTldIVv\GWwdDDJd4MtKHKnZ3Hy[Ixme3Nib3[gdJJqd3JiYXTtbY5qe3S{YYTpc44hd2ZiQ2PF Mm\hNlI4PjhzM{C=
HBE  NV3vT4ozTnWwY4Tpc44hSXO|YYm= NY[5dpBPOTBiwsXN NXm4ZW55eGG{dHnhcIx6KHKnc4TvdoV{KGSncHzleIlwdiCxZjDBV2wh\GWydHigbY4hS1OHIITy[YF1\WRibX;uc4xigWW{cx?= NIDYeIYzOjd4OEGzNC=>

... Click to View More Cell Line Experimental Data

Protocol

Solubility (25°C)

In vitro DMSO 78 mg/mL (198.73 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo

* 1 mg/ml means slightly soluble or 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
Formula

C24H28N2O3

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
NCT02951195 Recruiting Cystic Fibrosis Vertex Pharmaceuticals Incorporated November 2016 Phase 2
NCT03029455 Recruiting Cystic Fibrosis Vertex Pharmaceuticals Incorporated November 2016 Phase 1
NCT02934698 Enrolling by invitation Cystic Fibrosis Medical University of South Carolina|Vertex Pharmaceuticals Incorporated October 2016 Phase 3
NCT02953314 Recruiting Cystic Fibrosis Vertex Pharmaceuticals Incorporated October 2016 Phase 3
NCT02951182 Recruiting Cystic Fibrosis Vertex Pharmaceuticals Incorporated October 2016 Phase 2
NCT02730208 Recruiting Cystic Fibrosis Vertex Pharmaceuticals Incorporated September 2016 Phase 2

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CFTR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID