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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
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 is a FASN inhibitor which significantly reduces tubulin palmitoylation and mRNA expression.
Triheptanoin (IND106011; UX007) is a fatty acid metabolic modulator.
Rimiducid (AP1903) is a lipid-permeable tacrolimus analogue acts by cross-linking the FKBP domains.
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 is an enantiomer of C75, which is a synthetic fatty-acid synthase (FASN) inhibitor.
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