GLPG 0974

Modify Date: 2024-01-06 00:27:39

GLPG 0974 Structure
GLPG 0974 structure
Common Name GLPG 0974
CAS Number 1391076-61-1 Molecular Weight 485.00
Density N/A Boiling Point N/A
Molecular Formula C25H25ClN2O4S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of GLPG 0974


GLPG0974 is a free fatty acid receptor-2 (FFA2/GPR43) antagonist with an IC50 of 9 nM.

 Names

Name GLPG0974

 GLPG 0974 Biological Activity

Description GLPG0974 is a free fatty acid receptor-2 (FFA2/GPR43) antagonist with an IC50 of 9 nM.
Related Catalog
Target

IC50: 9 nM (GPR43)[1]

In Vitro GLPG0974 is able to inhibit acetate-induced neutrophil migration strongly in vitro and demonstrates ability to inhibit a neutrophil-based pharmacodynamic (PD) marker, CD11b activation-specific epitope [AE], in a human whole blood assay[1].
In Vivo GLPG0974 shows excellent pharmacokinetic properties in rat with a bioavailability of 47% and a linear increase of the plasma exposure after oral dosing at 5 and 30 mg/kg. The extended half-life observed following the increase of oral dose is consistent with the project objective to obtain long target coverage in human[1].
Animal Admin Rats[1] GLPG0974 is orally dosed as a single esophageal gavage at 5−10 mg/kg and intravenously dosed as a bolus via the caudal vein at 1 mg/kg to male Sprague−Dawley rats. Each group consisted of three rats. Blood samples are collected[1].
References

[1]. Pizzonero M, et al. Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic. J Med Chem. 2014 Dec 11;57(23):10044-57.

 Chemical & Physical Properties

Molecular Formula C25H25ClN2O4S
Molecular Weight 485.00
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