Ivacaftor benzenesulfonate

Modify Date: 2024-01-14 20:59:24

Ivacaftor benzenesulfonate structure	Common Name	Ivacaftor benzenesulfonate
	CAS Number	1134822-09-5	Molecular Weight	550.666
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₃₀H₃₄N₂O₆S	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Ivacaftor benzenesulfonate

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

Name	Ivacaftor benzenesulfonate
Synonym	More Synonyms

Description	Ivacaftor benzenesulfonate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment.
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> CFTR Research Areas >> Endocrinology
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 GABAA 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 IT in temperature-corrected F508del-FRT cells by appr 6-fold with an EC50 of 25 nM[4].
In Vivo	Ivacaftor (1-200 mg/kg, p.o.) exhibits good oral bioavailability in rat[3].
References	[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):9776-95 [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.

Molecular Formula	C₃₀H₃₄N₂O₆S
Molecular Weight	550.666
Exact Mass	550.213745
Storage condition	2-8℃

3-Quinolinecarboxamide, N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxo-, benzenesulfonate (1:1) (salt)

N-[5-Hydroxy-2,4-bis(2-methyl-2-propanyl)phenyl]-4-oxo-1,4-dihydro-3-quinolinecarboxamide benzenesulfonate (1:1)

Ivacaftor (benzenesulfonate)

DC Chemicals Limited
China
Product Name: Ivacaftor benzenesulfonate
Price: $Inquiry/25mg $Inquiry/50mg $Inquiry/100mg
Purity: 98.0%
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Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: Kalydeco benzenesulfonate
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

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Ivacaftor benzenesulfonate

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