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.
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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Citations for GLPG 0974
The citations listed below are publications that use Tocris products. Selected citations for GLPG 0974 include:
2 Citations: Showing 1 - 2
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Acetate coordinates neutrophil and ILC3 responses against C. difficile through FFAR2.
Authors: Marco Et al.
J Exp Med 2020;217
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Leuconostoc mesenteroides fermentation produces butyric acid and mediates Ffar2 to regulate blood glucose and insulin in type 1 diabetic mice.
Authors: Tsung-Hsien Et al.
Sci Rep 2020;10:7928
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