| Bioactivity | GLPG0974 is a free fatty acid receptor-2 (FFA2/GPR43) antagonist with an IC50 of 9 nM. | ||||||||||||
| Target | IC50: 9 nM (GPR43) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | GLPG0974 | ||||||||||||
| CAS | 1391076-61-1 | ||||||||||||
| Formula | C25H25ClN2O4S | ||||||||||||
| Molar Mass | 485.00 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Pizzonero M, et al. Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic. J Med Chem. 2014 Dec 11;57(23):10044-57. |