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ONO-8711
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
ONO-8711图片
CAS NO:216158-34-8
包装与价格：
包装价格(元)
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ONO-8711 是一种有效的选择性竞争性 EP1 受体拮抗剂（人和小鼠 EP1 的 Ki 分别为 0.6 和 1.7 nM）。 ONO-8711 有效降低结肠癌、乳腺癌和口腔癌小鼠模型中的肿瘤发病率和多样性。
Cas No.216158-34-8
别名(5Z)-6-[(2R,3S)-3-[[[(4-氯-2-甲基苯基)磺酰基]氨基]甲基]双环[2.2.2]辛-2-基]-5-己烯酸
化学名6-[(2R,3S)-3-[[[(4-chloro-2-methylphenyl)sulfonyl]amino]methyl]bicyclo[2.2.2]oct-2-yl]-5Z-hexenoic acid
Canonical SMILESClC1=CC(C)=C(S(N([H])C[C@@H](C2CCC3CC2)[C@H]3/C=C\CCCC(O)=O)(=O)=O)C=C1
分子式C22H30ClNO4S
分子量439.2
溶解度≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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).

 
 
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