GLPG0974 是 FFA2/GPR43 的拮抗剂，IC50 为 9 nM。

GLPG0974 is an antagonist of FFA2/GPR43 with IC50 of 9 nM.

GLPG0974 inhibits acetate-induced neutrophil migration strongly and inhibits CD11b activation-specific epitope [AE], a neutrophil-based pharmacodynamic marker, in a human whole blood assay[1].

GLPG0974(5 and 30 mg/kg; oral) exhibits good pharmacokinetic properties in rat with a bioavailability of 47% and dose-dependently increases the plasma exposure[1].

1391076-61-1

C25H25ClN2O4S

485

GLPG-0974

DMSO:180mg/mL (371.1mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years