ONO-8711
ONO-8711 is a potent and selective competitive antagonist of EP1 receptor (Ki = 0.6 and 1.7 nM for human and mouse EP1 respectively). ONO-8711 effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer.
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- No. CAS: 216158-34-8
- Fòrmula: C22H30ClNO4S
- Peso molecular:440.00
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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EP |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Sprague-Dawley rats (induced breast cancer by gavage of 85 mg/kg PhIP (HY-118716) 4 times for 2 weeks)
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Dosage:400 or 800 p.p.m.
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Administration:p.o.; for 20 weeks
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Result:Did not induce any symptoms of toxicity at 800 p.p.m..
Delayed occurrence of breast tumors for 2 or 4 weeks at 400 or 800 p.p.m., respectively.
Significantly suppressed cancer incidence compared with the control diet group at 800 p.p.m. (56% versus 79%, P < 0.05).
Chemical Information
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No. CAS 216158-34-8
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Peso molecular 440.00
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Fòrmula C22H30ClNO4S
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SMILES
O=C(O)CCC/C=C\[C@H]1C(CC2)CCC2[C@@H]1CNS(=O)(C3=CC=C(Cl)C=C3C)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ONO-8711 Related Classifications
HY-12182 Related Classifications
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