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Ivacaftor benzenesulfonate

Catalog No. T13742 CAS 1134822-09-5

Synonyms: VX-770 benzenesulfonate

Ivacaftor benzenesulfonate used for cystic fibrosis treatment. is an orally bioavailable CFTR potentiator.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Ivacaftor benzenesulfonate Chemical Structure

Ivacaftor benzenesulfonate, CAS 1134822-09-5

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 1,520.00
50 mg	6-8 weeks	$ 1,980.00
100 mg	6-8 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Ivacaftor benzenesulfonate used for cystic fibrosis treatment. is an orally bioavailable CFTR potentiator.
In vitro	Ivacaftor, at a concentration of 10 μM, significantly enhances CFTR activity in cells expressing the W1282X mutation, showing superior efficacy compared to cells with the R1162X mutation. It exhibits negligible activity towards 160 other targets, including the GABAA benzodiazepine receptor. Additionally, ivacaftor notably enhances chloride secretion, demonstrating a 10-fold increase in potency with an EC50 of 0.236 ± 0.200 μM compared to F508del HBEs. In recombinant cells, VX-770 (ivacaftor) markedly improves the CFTR channel's open probability (Po) in the presence of both F508del processing and G551D gating mutations, and amplifies forskolin-stimulated IT in temperature-corrected F508del-FRT cells approximately 6-fold at an EC50 of 25 nM. Ivacaftor triples PC secretion activity for the ABCB4-G535D mutation and significantly amplifies it for ABCB4-G536R (13.7-fold), ABCB4-S1076C (6.7-fold), ABCB4-S1176L (9.4-fold), and ABCB4-G1178S (5.7-fold), effectively correcting the functional defects of these ABCB4 mutations.
In vivo	Ivacaftor (1-200 mg/kg, p.o.) exhibits good oral bioavailability in rat.

Synonyms	VX-770 benzenesulfonate
Molecular Weight	550.67
Formula	C30H34N2O6S
CAS No.	1134822-09-5

Storage

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

References and Literature

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 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 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 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.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Ivacaftor benzenesulfonate 1134822-09-5 Others VX-770 benzenesulfonate inhibitor inhibit

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