cr 6086

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) 作为口服前列腺素 E2 (EP4) 受体拮抗剂，绑定 EP4 受体的能力强，Ki 值为 16.6 nM。该化合物能有效抑制 PGE2 诱导的 cAMP 生成，IC50 值达 22 nM，显示出显著的免疫调节和抗血管生成特性，对小鼠胶原诱导性关节炎的改善效果显著。