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873054-44-5

873054-44-5 structure
873054-44-5 structure
  • Name: Ivacaftor (VX-770)
  • Chemical Name: ivacaftor
  • CAS Number: 873054-44-5
  • Molecular Formula: C24H28N2O3
  • Molecular Weight: 392.491
  • Catalog: Pharmaceutical intermediate API intermediate
  • Create Date: 2018-10-03 07:43:33
  • Modify Date: 2024-01-02 23:43:51
  • 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
Synonyms 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
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
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

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title: CAS No. 873054-44-5 | Chemsrc address: https://m.chemsrc.com/en/baike/966700.html

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