873054-44-5

Solubility:DMSO

Storage:at -20℃ 2 years

Biologieal

VX-770 is a CFTR potentiator with an IC50 of 43 ± 38 nM. In recombinant cells VX-770 increased CFTR channel open probability (P(o)) in both the F508del processing mutation and the G551D gating mutation. VX-770 also increased Cl(-) secretion in cultured human CF bronchial epithelia (HBE) carrying the G551D gating mutation on one allele and the F508del processing mutation on the other allele by approximately 10-fold, to approximately 50% of that observed in HBE isolated from individuals without CF. Furthermore, VX-770 reduced excessive Na(+) and fluid absorption to prevent dehydration of the apical surface and increased cilia beating in these epithelial cultures.

Reference

[1] Van Goor F et al. Proc Natl Acad Sci U S A. 2009 Nov 3;106(44):18825-30