GLPG1837 是一种有效的 CFTR 增强剂，对其 F508del 和 G551D 的 EC50 分别为 3 nM 和 339 nM。

GLPG1837 is an effective 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 the obtained potency of 181 nM[1]. GLPG1837 is reversible CFTR potentiator, with the apparent affinity within a range of 0.2～2 μM[2].

CFBe41o- cells are cultured in Eagle's Minimal Essential Medium (MEM) supplemented with 10% fetal bovine serum (FBS), 1% penicillin/streptomycin, 1% l-glutamine, and 500 μg/mL hygromycin B. The cells are grown on culture flasks coated with 0.01% bovine serum albumin (BSA), 30 μg/mL Purecol, and 0.001% human fibronectin. CFBe41o- cells are transduced with adenoviruses containing F508del CFTR and YFP (H148Q/I152L/F47L). HEK293 cells are cultured in Dulbecco's Modified Eagle Medium (DMEM) supplemented with 10% FBS and 1% penicillin/streptomycin. HEK293 cells are transfected with plasmids containing G551D, G178R, S549N, R117H, CFTR, and YFP (H148Q/I152L/F47L). Directly after transfection, the HEK293 cells are seeded in black 96-well plates coated with poly-d-lysine at a density of 70000 cells per well. The next day, cells are incubated for 24 h at 27°C (CFBE41o?) or 37°C (HEK293). Then cells are treated for 10 min with 10 μM forskolin and the desired concentration of potentiator at room temperature.

1654725-02-6

C16H20N4O3S

348.42

ABBV-974

H2O:Insoluble
Ethanol:5 mg/mL
DMSO:60 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years