GLPG1837

GLPG1837 is a potentiator of cystic fibrosis transmembrane conductance regulator (CFTR).{52061,52059} It increases forskolin-induced opening of wild-type and mutant CFTRs expressing the F508 deletion (F508del) and G551D missense mutations with EC50 values of 88, 3, and 339 nM, respectively, in a reporter assay. GLPG1837 increases forskolin-induced conductivity of patient-derived bronchial epithelial cells expressing both F508del- and G551D-mutant CFTRs (EC50 = 159 nM in a transepithelial clamp circuit (TECC) assay).{52061}