| Bioactivity | Vorbipiprant (CR6086) is an EP4 receptor antagonist, serving as a targeted immunomodulator. Thus, Vorbipiprant is also a potential immune checkpoint inhibitor, to turn cold tumors into hot tumors. Vorbipiprant also antagonizes PGE2-stimulated cAMP production (IC50=22 nM). Vorbipiprant exhibit striking DMARD effects in rodents, and anti-inflammatory activity to inhibt immune-mediated inflammatory diseases[1][2]. |
| Target | Ki: 16.6 nM (human EP4 receptor) |
| Name | Vorbipiprant |
| CAS | 1417742-86-9 |
| Formula | C26H27F3N2O3 |
| Molar Mass | 472.50 |
| 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]. Caselli G, et al. Pharmacological characterisation of CR6086, a potent prostaglandin E2 receptor 4 antagonist, as a new potential disease-modifying anti-rheumatic drug. Arthritis Res Ther. 2018 Mar 1;20(1):39. [2]. Caselli G, Ferrari F, Piepoli T, et al. Combination of the EP4 antagonist CR6086 and anti-PD-1 monoclonal antibody inhibits tumor growth in a microsatellite stable colorectal cancer in mice[J]. Cancer Research, 2020, 80(16_Supplement): 2208-2208. |
Vorbipiprant
CAS: 1417742-86-9 F: C26H27F3N2O3 W: 472.50
Vorbipiprant (CR6086) is an EP4 receptor antagonist, serving as a targeted immunomodulator. Thus, Vorbipiprant is also a
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