tcsc0034220 GLPG1837

GLPG1837 is a potent and reversible CFTR potentiator, with EC₅₀s of 3 nM and 339 nM for F508del and G551D CFTR, respectively.

IC50 & Target: EC50: 3 nM (F508del CFTR), 339 nM (G551D CFTR)^[1]

In Vitro: GLPG1837 is a potent CFTR potentiator, with EC₅₀s of 3 nM and 339 nM for F508del and G551D CFTR, respectively. GLPG1837 increases the conductivity of the G551D CFTR channel with obtained potency of 181 nM^[1]. GLPG1837 is reversible CFTR potentiator, with a the apparent affinity within a range of 0.2∼2 µM^[2].