CAS: 1654725-02-6

N-(3-Carbamoyl-5,5,7,7-Tetramethyl-5,7-Dihydro-4H-Thieno[2,3-c]Pyran-2-Yl)-1H-Pyrazole-3-Carboxamide

GLPG1837 (ABBV-974) is an effective CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively.

GLPG 1837 is a small molecule potentiator, which is derived from a synthetic compound designed to target cystic fibrosis transmembrane conductance regulator (CFTR) protein variants. The source of GLPG 1837 is based on medicinal chemistry approaches focused on optimizing interactions with CFTR. The mode of action involves enhancing the channel gating of the CFTR protein, specifically addressing defects in CFTR function by increasing the probability of the channel being open and facilitating chloride ion transport across cell membranes. GLPG 1837 is primarily used in the context of cystic fibrosis (CF), a genetic disorder characterized by mutations in the CFTR gene leading to impaired ionic balance and accumulation of thick mucus in various organs. By facilitating chloride transport, GLPG 1837 aims to restore ion flow and mitigate respiratory, gastrointestinal, and pancreatic dysfunction associated with CF. Its applications are highly specific to particular CFTR mutations, making it a targeted therapeutic approach for certain subpopulations of CF patients.

GLPG1837