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Ivacaftor

Catalog No. T2588 CAS 873054-44-5

Synonyms: Ivacaftor (VX-770), VX-770

Ivacaftor (VX-770) (VX-770) is a potentiator of CFTR targeting G551D-CFTR (EC50: 100 nM) and F508del-CFTR (EC50: 25 nM) in Fisher rat thyroid cells, respectively.

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Ivacaftor, CAS 873054-44-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 32.00
5 mg	In stock	$ 74.00
10 mg	In stock	$ 129.00
25 mg	In stock	$ 216.00
50 mg	In stock	$ 319.00
100 mg	In stock	$ 479.00
500 mg	In stock	$ 1,050.00
1 mL * 10 mM (in DMSO)	In stock	$ 81.00

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Purity: 99%

Purity: 98%

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Description	Ivacaftor (VX-770) (VX-770) is a potentiator of CFTR targeting G551D-CFTR (EC50: 100 nM) and F508del-CFTR (EC50: 25 nM) in Fisher rat thyroid cells, respectively.
Targets&IC50	CFTR (G551D):100 nM(EC50, Fisher rat thyroid cells), F508del CFTR:25 nM(EC50, Fisher rat thyroid cells)
In vitro	VX-770 increased the forskolin-stimulated IT in temperature-corrected F508del-FRT cells by ~6-fold with an EC50 of 25 ± 5 nM. Before the addition of VX-770, the CFTR channel was exposed to maximally effective concentrations of PKA (75 nM) and ATP (1 mM). Under these conditions, 10 μM VX-770 increased the Po of G551D CFTR by ~6-fold [1]. HEK293 cells transiently expressing ABCB4-wt or the mutants were treated with 10 μmol/L of ivacaftor (VX-770), for 24 hours. Treatment with ivacaftor increased 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 [2].
In vivo	In a rat dose proportionality study, the AUC and Cmax were increased linearly after oral administration of Ivacaftor in a suspension vehicle at doses from 1 to 200 mg/kg (3, 10, 30, and 100 were the intermediate doses). A similar trend was observed in beagle dogs increasing the oral dose from 3 to 80 mg/kg (10, 30, and 60 were the intermediate doses), confirming high levels of oral absorption. The predicted human hepatic clearance of Ivacaftor using allometric scaling from four species was 4.7 mL min?1 kg?1, which is approximately 23% of hepatic blood flow [3].
Cell Research	HEK293 cells were seeded on poly-lysine precoated six-well plates at a density of 1.3 x 10^6 cells/well. Six hours after seeding, cells were transiently transfected with 1μg of ABCB4-encoding plasmids using Turbofect, following the manufacturer's instructions. Twenty-four hours post-transfection, cells were washed twice with HBSS, then the medium was replaced by phenol red-free DMEM containing 0.5 mmol/L sodium taurocholate and 0.02% fatty acid–free bovine serum albumin (BSA) in the presence or absence of 10 μmol/L of ivacaftor, 50 μM/L of UDCA, and 10 μmol/L of ivacaftor plus 50 μM/L of UDCA. Media were collected after 24 hours [2].
Animal Research	Male mouse,Sprague?Dawley rats,beagle dog,and cynomolgus monkeys (n = 3/group) were administered a single iv dose of compound formulated in dimethyl isosorbide/ethanol/PEG400/5% dextrose in water (D5W) (10%/15%/35%/40%) at the nominal dose indicated in a dose volume of 1 mL/kg.Blood samples (0.3 mL,sodium heparin anticoagulant) were collected from an indwelling carotid cannula at the following nominal time points: at predose,5,15,30,and 45 min and 1,2,4,6,8,12,24,36,and 48 h following iv administration and at predose,0.25,0.50,1,1.5,2,4,8,12,and 24 h following oral administration.The concentration of compound in the plasma samples was determined with a liquid chromatography/tandem mass spectrometry (LC/MS/MS) method,which had a lowest limit of quantitation (LLOQ) of 1 ng/mL and a linearity range between 1 and 2500 ng/mL [3].

Synonyms	Ivacaftor (VX-770), VX-770
Molecular Weight	392.49
Formula	C24H28N2O3
CAS No.	873054-44-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 72 mg/mL (183.4 mM)

References and Literature

1. 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. 2. 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. 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.

Citations

1. Sondo E, Cresta F, Pastorino C, et al. The L467F-F508del Complex Allele Hampers Pharmacological Rescue of Mutant CFTR by Elexacaftor/Tezacaftor/Ivacaftor in Cystic Fibrosis Patients: The Value of the Ex Vivo Nasal Epithelial Model to Address Non-Responders to CFTR-Modulating Drugs. International Journal of Molecular Sciences. 2022, 23(6): 3175. 2. Baldassarri M, Zguro K, Tomati V, et al.Gain-and Loss-of-Function CFTR Alleles Are Associated with COVID-19 Clinical Outcomes.Cells.2022, 11(24): 4096. 3. Tomati V, Costa S, Capurro V, et al.Rescue by elexacaftor-tezacaftor-ivacaftor of the G1244E cystic fibrosis mutation's stability and gating defects are dependent on cell background.Journal of Cystic Fibrosis.2022

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library EMA Approved Drug Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Target-Focused Phenotypic Screening Library CNS-Penetrant Compound Library Anti-Cancer Compound Library Orally Active Compound Library

Related Products

Related compounds with same targets

(R)-Elexacaftor CFTR corrector 8 VRT-532 GLPG1837 KM11060 Lumacaftor Glibenclamide Tezacaftor

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Keywords

Ivacaftor 873054-44-5 Autophagy Membrane transporter/Ion channel CFTR Ivacaftor (VX-770) Cystic fibrosis transmembrane conductance regulator inhibit VX-770 VX 770 Inhibitor VX770 inhibitor

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