Chemical Structure : Ivacaftor benzenesulfonate
CAS No.:
1134822-09-5
Ivacaftor benzenesulfonate
(VX-770 benzenesulfonate;VX 770 benzenesulfonate;VX770 benzenesulfonate)
Catalog No.: PC-43326Not For Human Use, Lab Use Only.
Ivacaftor (VX-770, VX770) is a potent, orally bioavailable CFTR potentiator, increases G551D- and F508del CFTR-mediated Cl- secretion with EC50 of 100 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
Ivacaftor (VX-770, VX770) is a potent, orally bioavailable CFTR potentiator, increases G551D- and F508del CFTR-mediated Cl- secretion with EC50 of 100 nM; increases CFTR channel open probability (Po) in both the F508del processing mutation and the G551D gating mutation in recombinant cells, increases the Po of G551D CFTR by 6-fold, the Po of F508del- and wild-type CFTR by 5-fold and 2-fold, respectively; also potentiates CFTR-mediated Cl− secretion in primary cultures of G551D/F508del HBE and F508del HBE; demonstrates potential for treatment of cystic fibrosis with certain mutations in CFTR gene (primarily the G551D mutation).
Fibrosis
Approved
Physicochemical Properties
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M.Wt
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550.6658
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Formula
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C30H34N2O6S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20 °C 12 Months; 4°C 6 Months
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- In Solvent
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-80 °C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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3-Quinolinecarboxamide, N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxo-, benzenesulfonate (1:1)
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References
1. Van Goor F, et al. Proc Natl Acad Sci U S A. 2009 Nov 3;106(44):18825-30.
2. Accurso FJ, et al. N Engl J Med. 2010 Nov 18;363(21):1991-2003.
3. Yu W, et al. J Biol Chem. 2011 Jul 15;286(28):24714-25.
4. Hadida S, et al. J Med Chem. 2014 Dec 11;57(23):9776-95.
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