ONO-8711
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 1mg | ¥1859.00 | 10-15工作日发货 | |
| 5mg | ¥5580.00 | 10-15工作日发货 | |
| 10mg | ¥8905.00 | 10-15工作日发货 | |
| 25mg | ¥15896.00 | 10-15工作日发货 |
特色产品
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
产品描述
ONO-8711 is a novel and selective EP1 antagonist.
Prostaglandin (PG) E2 functions by acting on a group of G-protein-coupled receptors (GPCRs) EP receptros. The EP receptors exhibit differences in signal transduction, tissue localization, and regulation of expression. The EP receptors have been implicated in various physiological and pathophysiological functions [2].
In vitro: In human pulmonary vessels, ONO-8711 (30 μM) non-competitively blocked the contractions produced with sulprostone, an EP1,3 agonist [3].
In vivo: In azoxymethane-treated C57BL/6J mice, administration of 250, 500, or 1000 ppm of ONO-8711 dose-dependently reduced ACF formation. In Min mice with a nonsense mutation in the adenomatous polyposis coli gene, treatment with 500 ppm ONO-8711 significantly reduced the number of intestinal polyps [1]. In female SD rats given PhIP, administration of ONO-8711 at 400 or 800 p.p.m. delayed occurrence of breast tumors for 2 or 4 weeks, respectively [4]. Treatment with ONO-8711 (800 p.p.m.) significantly decreased PhIP-induced breast cancer incidence, multiplicity and volume when compared with those of control rats [4].
References:
[1] Watanabe K, Kawamori T, Nakatsugi S, et al. Role of the prostaglandin E receptor subtype EP1 in colon carcinogenesis[J]. Cancer research, 1999, 59(20): 5093-5096.
[2] Sugimoto Y, Narumiya S. Prostaglandin E receptors[J]. Journal of Biological Chemistry, 2007, 282(16): 11613-11617.
[3] Norel X, de Montpreville V, Brink C. Vasoconstriction induced by activation of EP 1 and EP 3 receptors in human lung: effects of ONO-AE-248, ONO-DI-004, ONO-8711 or ONO-8713[J]. Prostaglandins & other lipid mediators, 2004, 74(1): 101-112.
[4] Kawamori T, Uchiya N, Nakatsugi S, et al. Chemopreventive effects of ONO-8711, a selective prostaglandin E receptor EP1 antagonist, on breast cancer development[J]. Carcinogenesis, 2001, 22(12).
产品性质
| 物理外观 | A solid |
| CAS号 | 216158-34-8 |
| 分子式 | C22H30ClNO4S |
| 分子量 | 439.2 |
| 化学名称 | 6-[(2R,3S)-3-[[[(4-chloro-2-methylphenyl)sulfonyl]amino]methyl]bicyclo[2.2.2]oct-2-yl]-5Z-hexenoic acid |
| 溶解度 | ≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide |
| SMILES | Cc(cc(cc1)Cl)c1S(NC[C@@H](C1CCC2CC1)[C@H]2/C=C\CCCC(O)=O)(=O)=O |
| 存储条件 | -20°C |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献,APExBIO并未验证,仅供参考)
IC50和靶点
| 生物活性描述 | ONO-8711 是一种强效、选择性的 EP1 受体竞争性拮抗剂,对人类和小鼠 EP1 的 Kis 值分别为 0.6 nM 和 1.7 nM。ONO-8711 能有效降低结肠癌、乳腺癌和口腔癌小鼠模型的肿瘤发病率和复发率。 |



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