I1421 is an activator of the cystic fibrosis transmembrane conductance regulator (CFTR), with an EC50 of 64 nM for WTCFTR currents. It also allosterically activates various CF-causing mutants, demonstrating good in vivo efficacy with an oral bioavailability of 60% in mice and a corresponding half-life of 75 minutes. I1421 works synergistically with Elexacaftor to enhance CFTR currents.
Formel:
C18H18FN3O3
Target-Kategorie:
CFTR
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