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ONO-8711 dicyclohexylamine

目录号 : GC67726

ONO-8711 dicyclohexylamine 是一种有效的选择性竞争性 EP1拮抗剂,对人和小鼠 EP1 的 Ki 值分别为 0.6 nM 和 1.7 nM。ONO-8711 dicyclohexylamine 有效降低结肠癌、乳腺癌和口腔癌小鼠模型的肿瘤发生率。

ONO-8711 dicyclohexylamine Chemical Structure

规格 价格 库存 购买数量
1mg
¥1,170.00
现货
5mg
¥3,690.00
现货
10mg
¥5,850.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

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].

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].

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: Female Sprague-Dawley rats (induced breast cancer by gavage of 85 mg/kg PhIP 4 times for 2 weeks)
Dosage: 400 or 800 p.p.m.
Administration: p.o.; for 20 weeks
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).

[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.

Chemical Properties

Cas No. SDF Download SDF
分子式 C34H53ClN2O4S 分子量 621.31
溶解度 DMSO : 50 mg/mL (80.48 mM; ultrasonic and warming and heat to 60°C) 储存条件 4°C, away from moisture
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.6095 mL 8.0475 mL 16.095 mL
5 mM 0.3219 mL 1.6095 mL 3.219 mL
10 mM 0.161 mL 0.8048 mL 1.6095 mL
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