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Chemical Structure : GLPG1205
Catalog No.: PC-72356Not For Human Use, Lab Use Only.
GLPG1205 is a potent and selective GPR84 inhibitor (negative allosteric modulator) with IC50 of 54 nM (hGPR84).
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GLPG1205 is a potent and selective GPR84 inhibitor (negative allosteric modulator) with IC50 of 54 nM (hGPR84).
GLPG1205 is fully selective over close homologs GPR43 (FFA2R) and GPR41 (FFA3R) and >100-fold selective over 123 other GPCRs on a Millipore GPCR Profiler panel.
GLPG1205 exhibits high potency in human and rat neutrophil assay with IC50 of 11 nM and 111 nM, respectively.
GLPG1205 (once-daily doses of 3 and 10 mg/kg) reduced disease activity index score and neutrophil infiltration in a mouse dextran sodium sulfate-induced chronic inflammatory bowel disease model, with efficacy similar to positive-control compound sulfasalazine.
| M.Wt | 378.428 | |
| Formula | C22H22N2O4 | |
| Appearance | Solid | |
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1. Labéguère F, et al. J Med Chem. 2020 Nov 25;63(22):13526-13545.
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