CJ-023423
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 5mg | ￥855.00 | 10-15工作日发货 | |
| 10mg | ￥1425.00 | 10-15工作日发货 | |
| 25mg | ￥2375.00 | 10-15工作日发货 |
特色产品
- 适用于流式细胞仪和荧光显微镜检测
- 准确区分活细胞/凋亡细胞/坏死细胞
- 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
- 对细胞无毒性
- 步骤更简单，无需有机溶剂
- 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
- 优异的扩增效率、可重复性和稳定性
- 卓越的灵敏度和准确性，操作简单
- 优化的缓冲液和T7 RNA聚合酶混合物
- 20 μL反应体系可获得更高的RNA产量
产品描述
Ki : 13 and 20 nM for human and rat EP4, respectively
CJ-023423 is an EP4 receptor antagonist.
Prostaglandin E2 (PGE2) can activate 4 E prostanoid (EP) receptors, namded EP1-4. EP4, a Gs protein-coupled receptor, plays key roles in cancer, bone formation and resorption, as well as atherosclerosis by elevating the second messenger cAMP.
In vitro: In vitro, CJ-023,423 was able to inhibit [(3)H]PGE(2) binding to both human and rat EP(4) receptors. CJ-023,423 was found to be highly selective for the human EP(4) receptor over other human prostanoid receptor subtypes. CJ-023,423 also inhibited PGE(2)-evoked elevation in intracellular cAMP at the human and rat EP(4) receptors with pA(2) of 8.3 and 8.2 nM, respectively [1].
In vivo: In vivo, po administration of CJ-023,423 could significantly reduce the thermal hyperalgesia that was induced by i.p. injection of PGE(2). CJ-023,423 was also effective in models of acute and chronic inflammatory pain. In addition, CJ-023,423 was able to significantly reduce mechanical hyperalgesia in the carrageenan model. Furthermore, CJ-023,423 reversed complete Freund's adjuvant-induced chronic inflammatory pain response significantly [1].
Clinical trial: A study of the effect of CJ-023,423 on the incidence of stomach ulcers has been completed but no result is release. Another phase II trial of CJ-023,423 in advanced solid tumors is proposed [https://clinicaltrials.gov/ct2/results term=CJ-023423&Search=Search].
Reference:
[1] Nakao, K. ,Murase, A.,Ohshiro, H., et al. CJ-023,423, a novel, potent and selective prostaglandin EP4 receptor antagonist with antihyperalgesic properties. Journal of Pharmacology and Experimental Therapeutics 322(2), 686-694 (2007).
产品性质
| 物理外观 | A crystalline solid |
| CAS号 | 415903-37-6 |
| 分子式 | C26H29N5O3S |
| 分子量 | 491.6 |
| 小分子别名 | Grapiprant |
| 化学名称 | N-[[2,4-(2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenylethylamino]carbonyl]-4-methyl-benzenesulfonamide |
| 溶解度 | ≤10mg/ml in ethanol;10mg/ml in DMSO;20mg/ml in dimethyl formamide |
| SMILES | O=C(NS(C1=CC=C(C)C=C1)(=O)=O)NCCC2=CC=C(N3C(CC)=NC4=C(C)N=C(C)C=C43)C=C2 |
| 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 | Grapiprant（CJ-023423）是一种选择性 EP4 受体拮抗剂，其生理配体为前列腺素 E2（PGE2）。Grapiprant 可取代[3H]-PGE2（1 nM）与狗重组 EP4 受体的结合，IC50 值为 35 nM，Ki 值为 24 nM。Grapiprant 具有治疗骨关节炎疼痛和炎症的潜力。 |
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