Free shipping on all orders over $ 500

GLPG0974

Cat. No. M10096
GLPG0974 Structure
Synonym:

GLPG-0974

Size Price Availability
10mg USD 680 1-2 Weeks
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98%
  • 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 484.99
Formula C25H25ClN2O4S
CAS Number 1391076-61-1
Purity >98%
Solubility
Storage at -20°C
References

Mouse Abdominal Fat Depots Reduced by Butyric Acid-Producing Leuconostoc mesenteroides
John Jackson Yang, et al. Microorganisms. 2020 Aug 3;8(8):1180. PMID: 32756446.

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
Meng Li, et al. Front Pharmacol. 2018 May 23;9:533. PMID: 29875665.

FFA2 activation combined with ulcerogenic COX inhibition induces duodenal mucosal injury via the 5-HT pathway in rats
Yasutada Akiba, et al. Am J Physiol Gastrointest Liver Physiol. 2017 Aug 1;313(2):G117-G128. PMID: 28526687.

Safety, pharmacokinetics and pharmacodynamics of GLPG0974, a potent and selective FFA2 antagonist, in healthy male subjects
Florence Namour, et al. Br J Clin Pharmacol. 2016 Jul;82(1):139-48. PMID: 26852904.

Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic
Mathieu Pizzonero, et al. J Med Chem. 2014 Dec 11;57(23):10044-57. PMID: 25380412.

Related FAS Products
TVB-3664

TVB-3664 is a FASN inhibitor which significantly reduces tubulin palmitoylation and mRNA expression.

Triheptanoin

Triheptanoin (IND106011; UX007) is a fatty acid metabolic modulator.

AP1903 (Rimiducid)

Rimiducid (AP1903) is a lipid-permeable tacrolimus analogue acts by cross-linking the FKBP domains.

Fatostatin

Fatostatin A is a cell permeable inhibitor of SREBP activation, it inhibits cancer cell proliferation by affecting mitotic microtubule spindle assembly and cell division.

C75 trans

C75 trans is an enantiomer of C75, which is a synthetic fatty-acid synthase (FASN) inhibitor.

  Catalog
Abmole Inhibitor Catalog 2017




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

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.