Art. -Nr.: HY-13017

Ivacaftor

(Synonyms: VX-770)

29 Cited Publications

Kundenbewertung

Based on 29 publication(s) in Google Scholar

Ivacaftor (VX-770) is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC₅₀s of 100 nM and 25 nM, respectively.

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Reinheit: 99.97%
CAS. Nr.: 873054-44-5
Formel: C₂₄H₂₈N₂O₃
Molecular Weight:392.49

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Ivacaftor Chemical Structure

CAS. Nr.: 873054-44-5

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (29)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Ivacaftor (VX-770) is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC₅₀s of 100 nM and 25 nM, respectively.

IC₅₀ & Target

EC50: 100 nM (G551D-CFTR), 25 nM (F508del-CFTR)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
Epithelial cell	EC₅₀	0.236 μM Compound: 48	Potentiation of human CFTR F508del mutant in human bronchial epithelial cells by Ussing chambers recording technique Potentiation of human CFTR F508del mutant in human bronchial epithelial cells by Ussing chambers recording technique	[PMID: 25441013]
Epithelial cell	EC₅₀	22 nM Compound: 48	Potentiation of human CFTR F508del/G551D mutant in human bronchial epithelial cells by Ussing chambers recording technique Potentiation of human CFTR F508del/G551D mutant in human bronchial epithelial cells by Ussing chambers recording technique	[PMID: 25441013]
NIH3T3	EC₅₀	3 nM Compound: 48	Potentiation of human CFTR F508del mutant expressed in mouse NIH-3T3 cells after 30 mins by fluorescent voltage sensing optical assay Potentiation of human CFTR F508del mutant expressed in mouse NIH-3T3 cells after 30 mins by fluorescent voltage sensing optical assay	[PMID: 25441013]
NRK-49F	IC₅₀	4 μM Compound: Ivacaftor	Inhibition of TGF-beta1-induced total collagen accumulation in rat NRK-49F cells Inhibition of TGF-beta1-induced total collagen accumulation in rat NRK-49F cells	[PMID: 25467157]
Vero	CC₅₀	27.34 μM Compound: Ivacaftor	Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr	10.1101/2020.03.20.999730
Vero	IC₅₀	6.57 μM Compound: Ivacaftor	Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr	10.1101/2020.03.20.999730

In Vitro

Ivacaftor (10?μM) increases the PC secretion activity by 3-fold for ABCB4-G535D, 13.7-fold for ABCB4-G536R, 6.7-fold for ABCB4-S1076C, 9.4-fold for ABCB4-S1176L, and 5.7-fold for ABCB4-G1178S. Ivacaftor corrects the functional defect of ABCB4 mutants^[1]. Ivacaftor (10 μM) significantly increases CFTR activity in W1282X-expressing cells compared to R1162X CFTR cells^[2]. Ivacaftor shows no significant activity against 160 targets tested including the GABA_A benzodiazepine receptor. Ivacaftor increases the chloride secretion with an EC₅₀ of 0.236 ± 0.200 μM, a 10-fold shift in potency compared to the F508del HBEs^[3]. In recombinant cells, VX-770 increases CFTR channel open probability (Po) in both the F508del processing mutation and the G551D gating mutation. VX-770 increases forskolin-stimulated I_T in temperature-corrected F508del-FRT cells by appr 6-fold with an EC₅₀ of 25 nM^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Ivacaftor (1-200 mg/kg, p.o.) exhibits good oral bioavailability in rat^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 873054-44-5
Appearance Solid
Molecular Weight 392.49
Formel C₂₄H₂₈N₂O₃
Color White to off-white
SMILES

CC(C)(C1=C(C=C(C(C(C)(C)C)=C1)O)NC(C2=CNC3=C(C2=O)C=CC=C3)=O)C
Synonyms

VX-770
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (29)

All Cell Proliferation/Viability AssayCell Imaging/StainingApoptosis AnalysisWBFlow Cytometry

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Journal Impact Factor

Acta Pharmacol Sin

Ivacaftor, a CFTR potentiator, synergizes with osimertinib against acquired resistance to osimertinib in NSCLC by regulating CFTR-PTEN-AKT axis. [Abstract]

2025 Apr;46(4):1045-1057. PMID: 39627385
Biomed Pharmacother

CFTR potentiator ivacaftor protects against noise-induced hair cell loss by increasing Nrf2 and reducing oxidative stress. [Abstract]

2023 Oct:166:115399. PMID: 37657258

Ivacaftor purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2023 Oct:166:115399. [Abstract]

Treatment with Ivacaftor (5 μM) prevents the decrease of CFTR and the increase of p-CFTR (S737) after noise exposure in OHCs.

Ivacaftor purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2023 Oct:166:115399. [Abstract]

Representative immunoblots show CFTR and p-CFTR (S737) with or without hydrogen peroxide or ivacaftor treatment versus DMSO alone (control). HEI-OC1 cells were pretreated with 5 μM Ivacaftor or equal concentration of DMSO for 12 h then treated with or without exposure to 10 mM hydrogen peroxide for 15 min.

Ivacaftor purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2023 Oct:166:115399. [Abstract]

ROS detection by DCFH-DA flow cytometry shows an increase in ROS accumulation after hydrogen peroxide stimulation of HEI-OC1 cells, while pretreatment with Ivacaftor (5 μM) blocks this effect.
JCI Insight

Targeting PI3Kγ anchoring enhances CFTR membrane localization and modulator efficacy via PKD1. [Abstract]

2026 Mar 23;11(6):e198846. PMID: 41869727
J Cyst Fibros

A functional comparison of vanzacaftor/tezacaftor/deutivacaftor and elexacaftor/tezacaftor/ivacaftor in patient-derived intestinal organoids with rare CFTR variants. [Abstract]

2026 Jun 16:S1569-1993(26)01643-7. PMID: 42303492
Am J Respir Cell Mol Biol

Distinct Responses of Cystic Fibrosis Epithelial Cells to SARS-CoV-2 and Influenza A Virus. [Abstract]

2025 Mar;72(3):308-319. PMID: 39311876
Cells

Mitochondrial Fragmentation Induced by the CFTR Modulators Lumacaftor and Ivacaftor in Immortalized Cystic Fibrosis Cell Lines. [Abstract]

2025 Oct 15;14(20):1601. PMID: 41148816
Int J Mol Sci

Restoration of Defective CFTR in Human Nasal Respiratory Epithelial Cells by CFTR Modulators and mRNA Transfection. [Abstract]

2026 Feb 23;27(4):2063. PMID: 41752197
Int J Mol Sci

Assessing CFTR Function and Epithelial Morphology in Human Nasal Respiratory Cell Cultures: A Combined Immunofluorescence and Electrophysiological Study. [Abstract]

2025 Aug 6;26(15):7618. PMID: 40806745
J Mol Struct

2025 Nov 10;1353:144673.
Am J Physiol Cell Physiol

Modeling ocular surface ion and water transport by generation of lipid- and mucin-producing human meibomian gland and conjunctival epithelial cells. [Abstract]

2025 Mar 1;328(3):C856-C871. PMID: 39870373
Front Cell Dev Biol

Ivacaftor Inhibits Glioblastoma Stem Cell Maintenance and Tumor Progression. [Abstract]

2021 May 11:9:678209. PMID: 34046412

Ivacaftor purchased from MedChemExpress. Usage Cited in: Front Cell Dev Biol. 2021 May 11:9:678209. [Abstract]

The cells proliferation of GSC11 (left panel) and GBM1 (right panel) treated by 5 μM Ivacaftor.

Ivacaftor purchased from MedChemExpress. Usage Cited in: Front Cell Dev Biol. 2021 May 11:9:678209. [Abstract]

Ivacaftor (5 μM) treatment significantly increases cellular apoptosis in GSC11 and GBM1 cells determined by flow cytometry assay.
Ther Adv Med Oncol

Repurposing of ivacaftor shows potential to treat ROR1 expressing high-grade serous ovarian cancer. [Abstract]

2026 Jan 2:18:17588359251409010. PMID: 41487693
Hum Gene Ther

SP-101, A Novel Adeno-Associated Virus Gene Therapy for the Treatment of Cystic Fibrosis, Mediates Functional Correction of Primary Human Airway Epithelia From Donors with Cystic Fibrosis. [Abstract]

2024 Sep;35(17-18):695-709. PMID: 39155805
Sci Rep

CFTR acts as a potential therapeutic target for attention deficit-hyperactivity disorder. [Abstract]

2025 Apr 21;15(1):13767. PMID: 40258939
Biomedicines

Rescue of Mutant CFTR Channel Activity by Investigational Co-Potentiator Therapy. [Abstract]

2025 Jan 1;13(1):82. PMID: 39857666
J Biol Chem

A nonnatural peptide targeting the A-kinase anchoring function of PI3Kγ for therapeutic cAMP modulation in pulmonary cells. [Abstract]

2024 Nov;300(11):107873. PMID: 39393573
Microbiol Spectr

Condition-dependent effects of Elexacaftor/Tezacaftor/Ivacaftor (Trikafta) on Aspergillus fumigatus growth. [Abstract]

2025 Sep 2;13(9):e0227524. PMID: 40736245
PNAS Nexus

VX-445 (elexacaftor) inhibits chloride secretion across human bronchial epithelial cells by directly blocking KCa3.1 channels. [Abstract]

2025 Jul 4;4(7):pgaf211. PMID: 40688096
J Cell Sci

Lipid-driven CFTR clustering is impaired in cystic fibrosis and restored by corrector drugs. [Abstract]

2022 Mar 1;135(5):jcs259002. PMID: 35060604
Am J Physiol Lung Cell Mol Physiol

Effect of elexacaftor and bamocaftor on the metabolic and thermal stability of the F508del-CFTR protein in human airway epithelial cells. [Abstract]

2025 Aug 13. PMID: 40803756
Org Process Res Dev

2019, 23, 11, 2302-2322.
Glycoconj J

Effects of GM1 ganglioside and its derivatives on ETI-rescued F508del-CFTR maturation and host-pathogen interactions in cystic fibrosis bronchial cells. [Abstract]

2025 Aug;42(3-4):173-186. PMID: 40663265
Glycoconj J

Effect of CFTR modulators Elexacaftor/Tezacaftor/Ivacaftor on lipid metabolism in human bronchial epithelial cells. [Abstract]

2025 Feb;42(1):1-14. PMID: 39797966
bioRxiv

Profiling the CFTR Variant Selectivity and Off-Target Interactions of VX-121. [Abstract]

2026 Jun 8:2026.06.01.729306. PMID: 42282787
University of Lisbon

2026.
bioRxiv

General Trends in the Calnexin-Dependent Expression and Pharmacological Rescue of Clinical CFTR Variants. [Abstract]

2025 Sep 11:2025.04.03.647093. PMID: 40964320
bioRxiv

Chronic pancreatitis patient-derived organoids reveal new paths to precision therapeutics. [Abstract]

2025 Nov 14:2024.10.30.620903. PMID: 41279927
bioRxiv

2024 August 16.
University of Kentucky

2022 Aug.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (127.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5478 mL

12.7392 mL

25.4784 mL

5 mM

0.5096 mL

2.5478 mL

5.0957 mL

10 mM

0.2548 mL

1.2739 mL

2.5478 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 3

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (6.37 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Delaunay JL, et al. Functional defect of variants in the adenosine triphosphate-binding sites of ABCB4 and their rescue by the cystic fibrosis transmembrane conductance regulator potentiator, ivacaftor (VX-770). Hepatology. 2017 Feb;65(2):560-570 [Content Brief]

[2]. Mutyam V, et al. Therapeutic benefit observed with the CFTR potentiator, ivacaftor, in a CF patient homozygous for the W1282X CFTR nonsense mutation. J Cyst Fibros. 2017 Jan;16(1):24-29 [Content Brief]

[3]. Hadida S, et al. Discovery of N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide (VX-770, ivacaftor), a potent and orally bioavailable CFTR potentiator. J Med Chem. 2014 Dec 11;57(23):9776-9 [Content Brief]

[4]. Van Goor F, et al. Rescue of CF airway epithelial cell function in vitro by a CFTR potentiator, VX-770. Proc Natl Acad Sci U S A. 2009 Nov 3;106(44):18825-30. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5478 mL	12.7392 mL	25.4784 mL	63.6959 mL
	5 mM	0.5096 mL	2.5478 mL	5.0957 mL	12.7392 mL
	10 mM	0.2548 mL	1.2739 mL	2.5478 mL	6.3696 mL
	15 mM	0.1699 mL	0.8493 mL	1.6986 mL	4.2464 mL
	20 mM	0.1274 mL	0.6370 mL	1.2739 mL	3.1848 mL
	25 mM	0.1019 mL	0.5096 mL	1.0191 mL	2.5478 mL
	30 mM	0.0849 mL	0.4246 mL	0.8493 mL	2.1232 mL
	40 mM	0.0637 mL	0.3185 mL	0.6370 mL	1.5924 mL
	50 mM	0.0510 mL	0.2548 mL	0.5096 mL	1.2739 mL
	60 mM	0.0425 mL	0.2123 mL	0.4246 mL	1.0616 mL
	80 mM	0.0318 mL	0.1592 mL	0.3185 mL	0.7962 mL
	100 mM	0.0255 mL	0.1274 mL	0.2548 mL	0.6370 mL

Keywords

Ivacaftor

29 Cited Publications

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Ivacaftor

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Publications Citing Use of MedChemExpress (MCE) Ivacaftor

Biologische Aktivität

Chemical Information

Publications (29)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Ivacaftor

Immunology/Inflammation Compound Library

Membrane Transporter/Ion Channel Compound Library

FDA-Approved Drug Library

Autophagy Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Drug-Induced Liver Injury (DILI) Compound Library

Rare Diseases Drug Library

Pediatric Drug Library

EMA-Approved Drug Library

Human Metabolite Library

Off-patent Drug Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Ivacaftor

Biologische Aktivität

Chemical Information

Publications (29)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Ivacaftor Related Classifications

HY-13017 Related Classifications