| Bioactivity | ONO-8711 dicyclohexylamine is a selective and orally active EP1 competitive antagonist with Ki value of 0.6 nM and 1.7 nM for human and mouse EP1 respectively. ONO-8711 dicyclohexylamine effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer[1]. |
| Target | Ki: 0.6 nM (human EP1), 1.7 nM (mouse EP1) |
| Invitro | ONO-8711 (10 and 30 μM; 30 min) blocks the contractions induced by sulprostone in human pulmonary veins in a non-competitive manner[2].ONO-8711 inhibits PGE2-induced increase in cytosolic Ca2+ concentration with IC50s of 0.21 μM, 0.05 μM, and 0.22 μM for the mouse, human, and rat receptors, respectively[3]. |
| In Vivo | ONO-8711 (400 or 800 p.p.m.; p.o.; for 20 weeks) suppresses cancer incidence and delays occurrence of breast tumors[3]. Animal Model: |
| Name | ONO-8711 dicyclohexylamine |
| Formula | C34H53ClN2O4S |
| Molar Mass | 621.31 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Watanabe K, et al. Role of the prostaglandin E receptor subtype EP1 in colon carcinogenesis. Cancer Res. 1999 Oct 15;59(20):5093-6. [2]. Norel X, et al. Vasoconstriction induced by activation of EP1 and EP3 receptors in human lung: effects of ONO-AE-248, ONO-DI-004, ONO-8711 or ONO-8713. Prostaglandins Other Lipid Mediat. 2004 Oct;74(1-4):101-12. [3]. Kawamori T, et al. Chemopreventive effects of ONO-8711, a selective prostaglandin E receptor EP(1) antagonist, on breast cancer development. Carcinogenesis. 2001 Dec;22(12):2001-4. |
ONO-8711 dicyclohexylamine
CAS: F: C34H53ClN2O4S W: 621.31
ONO-8711 dicyclohexylamine is a selective and orally active EP1 competitive antagonist with Ki value of 0.6 nM and 1.7 n
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