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Chemical Structure : Ivacaftor 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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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
| M.Wt | 550.6658 | |
| Formula | C30H34N2O6S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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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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