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CJ-023423
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。
CJ-023423图片
CAS NO:415903-37-6
规格:98%
分子量:491.6
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
EP4 receptor antagonist
CAS:415903-37-6
分子式:C26H29N5O3S
分子量:491.6
纯度:98%
存储:Store at -20°C

Background:

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).