Art. -Nr.: HY-13017B

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Ivacaftor hydrate

(Synonyms: VX-770 hydrate)

29 Cited Publications

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Based on 29 publication(s) in Google Scholar

Ivacaftor hydrate (VX-770 hydrate) is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment.

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CAS. Nr.: 1134822-07-3
Formel: C₂₄H₃₀N₂O₄
Molecular Weight:410.51

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

Ivacaftor hydrate Chemical Structure

CAS. Nr.: 1134822-07-3

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Publications (29)
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Ivacaftor hydrate (VX-770 hydrate) is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment.

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. 1134822-07-3
Molecular Weight 410.51
Formel C₂₄H₃₀N₂O₄
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.O
Synonyms

VX-770 hydrate
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (29)

All Cell Proliferation/Viability AssayCell Imaging/StainingApoptosis AnalysisWBFlow Cytometry

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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
JCI Insight

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

2026 Mar 23;11(6):e198846. PMID: 41869727
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 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 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
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
Front Cell Dev Biol

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

2021 May 11:9:678209. PMID: 34046412

Ivacaftor hydrate 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 hydrate 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.
J Mol Struct

2025 Nov 10;1353:144673.
Sci Rep

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

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

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

2025 Jan 1;13(1):82. PMID: 39857666
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
Microbiol Spectr

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

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

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

2025 Nov 14:2024.10.30.620903. PMID: 41279927
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

2024 August 16.
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 hydrate 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 hydrate 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 hydrate 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.
University of Kentucky

2022 Aug.

Reinheit & Dokumentation

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Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 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]

Calculators

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)}

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.

Keywords

Ivacaftor hydrate

29 Cited Publications

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Ivacaftor hydrate

Publications Citing Use of MedChemExpress (MCE) Ivacaftor hydrate

Biologische Aktivität

Chemical Information

Publications (29)

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

Ivacaftor hydrate Related Classifications

HY-13017B Related Classifications