Cat No.
CEI-0253
Description
VX-809 can inhibit CFTR with IC 50 of 100 nM.
CAS No.
936727-05-8
Targets
CFTR
Chemical Name
3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid
M.Wt
452.41
Purity
>99%
Solubility
DMSO 91 mg/mL Water
Storage
2 years at -20centigrade Powder
In vitro
VX-809 is a CFTR corrector that was advanced into clinical development for the treatment of cystic fibrosis. In cultured human bronchial epithelial cells isolated from patients with CF homozygous for F508del, VX-809 improved F508del-CFTR processing in the endoplasmic reticulum and enhanced chloride secretion to approximately 14% of non-CF human bronchial epithelial cells (EC(50), 81 +/- 19 nM), a level associated with mild CF in patients with less disruptive CFTR mutations. F508del-CFTR corrected by VX-809 exhibited biochemical and functional characteristics similar to normal CFTR, including biochemical susceptibility to proteolysis, residence time in the plasma membrane, and single-channel open probability.
