Ivacaftor (VX-770)

Modify Date: 2024-01-02 23:43:51

Ivacaftor (VX-770) structure	Common Name	Ivacaftor (VX-770)
	CAS Number	873054-44-5	Molecular Weight	392.491
	Density	1.2±0.1 g/cm3	Boiling Point	550.5±50.0 °C at 760 mmHg
	Molecular Formula	C₂₄H₂₈N₂O₃	Melting Point	N/A
	MSDS	N/A	Flash Point	286.7±30.1 °C

Use of Ivacaftor (VX-770)

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

Name	ivacaftor
Synonym	More Synonyms

Description	Ivacaftor is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively.
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> CFTR Research Areas >> Endocrinology
Target	EC50: 100 nM (G551D-CFTR), 25 nM (F508del-CFTR)[1]
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):9776-9 [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.

Density	1.2±0.1 g/cm3
Boiling Point	550.5±50.0 °C at 760 mmHg
Molecular Formula	C₂₄H₂₈N₂O₃
Molecular Weight	392.491
Flash Point	286.7±30.1 °C
Exact Mass	392.209991
PSA	85.68000
LogP	6.34
Vapour Pressure	0.0±1.5 mmHg at 25°C
Index of Refraction	1.606
Storage condition	2~8℃

HS Code	29333990

Precursor 9
CAS#:873055-58-4 5-Amino-2,4-bis... CAS#:1182822-31-6 5-Amino-2,4-di-... CAS#:13721-01-2 1,4-Dihydro-4-o... CAS#:1246213-45-5 Carbonic acid 5...
CAS#:96-76-4 2,4-Di-t-butylphenol CAS#:873055-54-0 Carbonic acid, ... CAS#:873055-55-1 2,4-Di-tert-but... CAS#:52980-28-6 Ethyl 4-hydroxy...
CAS#:54535-22-7 Propanedioic ac...
DownStream 2
CAS#:1246213-23-9 N-(2-(TERT-BUTY... CAS#:1246213-24-0 2-(5-(TERT-BUTY...

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

Ivacaftor

[14C]-Ivacaftor

Kalydeco

N-(2,4-ditert-butyl-5-hydroxyphenyl)-4-oxo-1H-quinoline-3-carboxamide

MFCD17171361

VX770

UNII-1Y740ILL1Z

N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxaraide

N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide

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

N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide

N-[2,4-Bis(tert-butyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxo-3-quinolinecarboxamide

VX-770

Shanghai Jizhi Biochemical Technology Co., Ltd
China
Product Name: Ivacaftor (VX-770)
Price: ￥698.0/50mg ￥248.0/10mg
Purity: 99.0%
Stocking Period: 1 Day
Contact: Liu jia

DC Chemicals Limited
China
Product Name: Ivacaftor (VX-770)
Price: $200.0/100mg $400.0/250mg $800.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Zhejiang Hangyu API Co., Ltd
China
Product Name: VX-770
Price: ￥Inquiry/1kg
Purity: 99.5%
Stocking Period: Inquiry
Contact: Vinnie

Henan Tianfu Chemical Co., Ltd.
China
Product Name: ivacaftor
Price: $Inquiry/1kg $Inquiry/25kg $Inquiry/1000kg $Inquiry/10ton
Purity: 99.0%
Stocking Period: Inquiry
Contact: Anson

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Price: ￥522.6/5mg

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