Description: |
CR6086 (CR-6086) is a potent, selective prostaglandin E2 receptor 4 (EP4) antagonist with Ki of 16.6 nM (hEP4 receptor), inhibits PGE2-stimulated cAMP production with IC50 of 22 nM; reduces key cytokine players of RA (IL-6 and VEGF expression in macrophages, IL-23 release from dendritic cells, IL-17 release from Th17 cells) in models of human immune cells in culture; significantly improves all features of arthritis: severity, histology, inflammation and pain in CIA models of RA in rats and mice; CR6086 is better than the selective COX-2 inhibitor rofecoxib and at least as effective as the JAK inhibitor tofacitinib. |