GLPG 0974

Cat. No. 5621

GLPG 0974 C25H25ClN2O4S [1391076-61-1]

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Chemical Name: 4-[[[(2R)-1-(Benzo[b]thien-3-ylcarbonyl)-2-methyl-2-azetidinyl]carbonyl][(3-chlorophenyl)methyl]amino]butanoic acid

Biological Activity

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

M.Wt:
485
Formula:
C25H25ClN2O4S
Solubility:
Soluble to 100 mM in DMSO and to 20 mM in 1eq. NaOH with gentle warming
Purity:
>98 %
Storage:
Store at +4°C
CAS No:
1391076-61-1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Pizzonero et al (2014) Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic. J.Med.Chem. 57 10044. PMID: 25380412.

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Keywords: GLPG 0974, supplier, GLPG0974, free, fatty, acid, receptors, FFA2, antagonists, antagonism, potent, Tocris Bioscience, Free Fatty Acid Receptor Antagonist products

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