GLPG0974,1391076-61-1

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GLPG0974

CAS No. : 1391076-61-1

MCE 国际站：GLPG0974

产品活性：GLPG0974是游离脂肪酸受体-2 (free fatty acid receptor-2 (FFA2/GPR43)) 拮抗剂，IC₅₀ 值为 9 nM。

研究领域：GPCR/G Protein

作用靶点：Free Fatty Acid Receptor

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.

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.

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