cr6086

CR6086 is a novel, potent EP4 antagonist showing favourable immunomodulatory properties, striking DMARD effects in rodents, and anti-inflammatory activity targeted to immune-mediated inflammatory diseases and distinct from the general effects of cyclooxygenase inhibitors. CR6086 showed selectivity and high affinity for the human EP4 receptor (Ki = 16.6 nM) and functioned as a pure antagonist (half-maximal inhibitory concentration, 22 nM) on PGE2-stimulated cAMP production.

ArgTX-48 is a highly potent and subfamily selective antagonist of the NMDARs and AMPARs.

(R)-Vorbipiprant ((R)-CR6086) is an orally effective antagonist of the prostaglandin E2 receptor 4 (EP4), demonstrating a Ki of 16.6 nM for human EP4. It inhibits the production of cAMP induced by PGE2, with an IC50 of 22 nM. Additionally, (R)-Vorbipiprant exhibits immunomodulatory and antiangiogenic activities, having shown potential to alleviate collagen-induced arthritis in mice.