GLPG 0974
Chemical Name: 4-[[[(2R)-1-(Benzo[b]thien-3-ylcarbonyl)-2-methyl-2-azetidinyl]carbonyl][(3-chlorophenyl)methyl]amino]butanoic acid
Purity: ≥98%
Biological Activity
GLPG 0974 is a 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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Background References
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Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
Pizzonero et al.
J.Med.Chem., 2014;57:10044
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