Chemical Structure : Ivacaftor hydrate
CAS No.:
1134822-07-3
Ivacaftor hydrate
(VX-770 hydrate;VX 770 hydrate;VX770 hydrate)
Catalog No.: PC-43327Not 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.
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
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
|
M.Wt
|
410.506
|
|
Formula
|
C24H30N2O4
|
|
Appearance
|
Solid
|
|
CAS No.
|
|
|
Storage
|
- Solide Powder
-
-20 °C 12 Months; 4°C 6 Months
|
- In Solvent
-
-80 °C 6 Months; -20°C 6 Months
|
|
Shipping
|
|
|
Solubility
|
10 mM in DMSO
|
|
Chemical Name/SMILES
|
3-Quinolinecarboxamide, N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxo-, hydrate (1:1)
|
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.
Contact Us
sales@probechem.com
