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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 216158-34-8
- 分子式: C22H30ClNO4S
- 分子量:440.00
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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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).
化学情報
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CAS 番号 216158-34-8
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分子量 440.00
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)