| CAS NO: | 415903-37-6 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Cas No. | 415903-37-6 |
| 别名 | RQ-00000007 |
| 化学名 | N-[[2,4-(2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenylethylamino]carbonyl]-4-methyl-benzenesulfonamide |
| Canonical 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 |
| 分子式 | C26H29N5O3S |
| 分子量 | 491.6 |
| 溶解度 | ≤10mg/ml in ethanol;10mg/ml in DMSO;20mg/ml in dimethyl formamide |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 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: |
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