GLPG0974

1391076-61-1

485.00

H2O : < 0.1 mg/mL (insoluble); DMSO : 200 mg/mL (412.37 mM; Need ultrasonic)

Others

GLPG0974 is a free fatty acid receptor-2 (FFA2/GPR43) antagonist with an IC₅₀ of 9 nM. IC50 & Target: IC50: 9 nM (GPR43)^[1] In Vitro: GLPG0974 is able to inhibit acetate-induced neutrophil migration strongly in vitro and demonstrates ability to inhibit a neutrophil-based pharmacodynamic (PD) marker, CD11b activation-specific epitope [AE], in a human whole blood assay^[1]. In Vivo: GLPG0974 shows excellent pharmacokinetic properties in rat with a bioavailability of 47% and a linear increase of the plasma exposure after oral dosing at 5 and 30 mg/kg. The extended half-life observed following the increase of oral dose is consistent with the project objective to obtain long target coverage in human^[1].