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  3. GLPG0974


Cat. No.: HY-12940
Handling Instructions

GLPG0974 is a free fatty acid receptor-2 (FFA2/GPR43) antagonist with an IC50 of 9 nM.

For research use only. We do not sell to patients.

GLPG0974 Chemical Structure

GLPG0974 Chemical Structure

CAS No. : 1391076-61-1

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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].

Clinical Trial
Molecular Weight







O=C(O)CCCN(C([[email protected]]1(C)N(C(C2=CSC3=CC=CC=C32)=O)CC1)=O)CC4=CC=CC(Cl)=C4


Room temperature in continental US; may vary elsewhere.


Please store the product under the recommended conditions in the Certificate of Analysis.

Animal Administration


GLPG0974 is orally dosed as a single esophageal gavage at 5−10 mg/kg and intravenously dosed as a bolus via the caudal vein at 1 mg/kg to male Sprague−Dawley rats. Each group consisted of three rats. Blood samples are collected[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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