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GLPG0974

Chemical Structure : GLPG0974

CAS No.: 1391076-61-1

GLPG0974 (GLPG-0974)

Catalog No.: PC-62591Not For Human Use, Lab Use Only.

GLPG 0974 is a potent, selective free fatty acid receptor 2 (FFA2, GPR43) antagonist with IC50 of 95 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GLPG0974 is a potent, selective free fatty acid receptor 2 (FFA2, GPR43) antagonist with IC50 of 95 nM.
GLPG0974 inhibits acetate-induced neutrophil migration strongly in vitro with IC50 of 27 nM.
GLPG0974 demonstrates ability to inhibit a neutrophil-based pharmacodynamic (PD) marker, CD11b activation-specific epitope [AE], in a human whole blood assay.

Physicochemical Properties

M.Wt 484.995
Formula C25H25ClN2O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-[[[(2R)-1-(Benzo[b]thien-3-ylcarbonyl)-2-methyl-2-azetidinyl]carbonyl][(3-chlorophenyl)

References

1. Pizzonero M, et al. J Med Chem. 2014 Dec 11;57(23):10044-57.

2. Sergeev E, et al. J Biol Chem. 2016 Jan 1;291(1):303-17.

3. Namour F, et al. Br J Clin Pharmacol. 2016 Jul;82(1):139-48.

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