| Bioactivity | ER-819762 is an orally active, highly selective prostaglandin E2 (PGE2) EP4 receptor antagonist with an EC50 of 70 nM against human EP4 receptor. ER-819762 can be used for rheumatoid arthritis research[1]. |
| Invitro | ER-819762 suppresses human EP4 receptor-mediated cell signalling as measured in a cAMP-dependent reporter assay (IC50 value of 59 ± 6 nM)[1].ER-819762 (0-10 μM, 3 days) selectively suppresses PGE2-induced Th1 differentiation[1].ER-819762 (0-5 μM, 24 h) suppresses IL-23 secretion in human monocyte-derived dendritic cells[1].ER-819762 (0.1 and 1 μM, 3 days) suppresses IL-17 production and inhibits IL-23-induced Th17 expansion in activated CD4+ T cells[1]. |
| In Vivo | ER-819762 (0-100 mg/kg; p.o.; daily) suppresses inflammatory arthritis in mice[1].ER-819762 (0-100 mg/kg; p.o.; once) suppresses CFA (Freund’s adjuvant)-induced hyperalgesia in rat[1]. Animal Model: |
| Name | ER-819762 |
| CAS | 1155773-15-1 |
| Formula | C30H39N3O3 |
| Molar Mass | 489.65 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Chen Q, et al. A novel antagonist of the prostaglandin E(2) EP(4) receptor inhibits Th1 differentiation and Th17 expansion and is orally active in arthritis models. Br J Pharmacol. 2010 May;160(2):292-310. |