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Chemical Structure : CR6086
Catalog No.: PC-20854Not For Human Use, Lab Use Only.
CR6086 (Vorbipiprant) 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.
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CR6086 (Vorbipiprant) 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.
CR6086 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.
CR6086 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.
| M.Wt | 472.51 | |
| Formula | C26H27F3N2O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Caselli G, et al. Arthritis Res Ther. 2018 Mar 1;20(1):39.
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