Potent FFA2 antagonist (IC50
= 9 nM). Exhibits selectivity for FFA2 over FFA3. Inhibits acetate-induced human neutrophil migration in plasma or buffer. Also inhibits FFA2-induced expression of CD11b activation-specific epitope (AE) in human whole blood. Orally bioavailable.
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All Tocris products are intended for laboratory research use only.
Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
Pizzonero et al.