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Cat. No. M10096
GLPG0974 Structure


Size Price Availability Quantity
10mg USD 340  USD340 In stock
25mg USD 460  USD460 In stock
50mg USD 920  USD920 In stock
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Quality Control & Documentation
  • Purity: >98%, ee.: 98.57%
  • COA
  • MSDS
Biological Activity

GLPG0974 is a potent and selective FFA2 (also called GPR43) antagonist with IC50 of 9 nM. GLPG0974 inhibits acetate-induced neutrophil migration strongly in vitro and demonstrated ability to inhibit a neutrophil-based pharmacodynamic (PD) marker, CD11b activation-specific epitope [AE], in a human whole blood assay.

Chemical Information
Molecular Weight 484.99
Formula C25H25ClN2O4S
CAS Number 1391076-61-1
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] John Jackson Yang, et al. Microorganisms. Mouse Abdominal Fat Depots Reduced by Butyric Acid-Producing Leuconostoc mesenteroides

[2] Meng Li, et al. Front Pharmacol. The Anti-inflammatory Effects of Short Chain Fatty Acids on Lipopolysaccharide- or Tumor Necrosis Factor α-Stimulated Endothelial Cells via Activation of GPR41/43 and Inhibition of HDACs

[3] Yasutada Akiba, et al. Am J Physiol Gastrointest Liver Physiol. FFA2 activation combined with ulcerogenic COX inhibition induces duodenal mucosal injury via the 5-HT pathway in rats

[4] Florence Namour, et al. Br J Clin Pharmacol. Safety, pharmacokinetics and pharmacodynamics of GLPG0974, a potent and selective FFA2 antagonist, in healthy male subjects

[5] Mathieu Pizzonero, et al. J Med Chem. Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic

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Keywords: GLPG0974, GLPG-0974 supplier, FAS, inhibitors, activators

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