CJ-023423
(Synonyms: RQ-00000007) 目录号 : GC10771
An EP4 receptor antagonist
Cas No.:415903-37-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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).
| Cas No. | 415903-37-6 | SDF | |
| 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°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0342 mL | 10.1709 mL | 20.3417 mL |
| 5 mM | 0.4068 mL | 2.0342 mL | 4.0683 mL |
| 10 mM | 0.2034 mL | 1.0171 mL | 2.0342 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。