CJ-42794
(Synonyms: 4-[(1S)-1-[[5-氯-2-(4-氟苯氧基)苄基]氨基]乙基]苯甲酸,RQ-00015986) 目录号 : GC13284
A selective EP4 receptor antagonist
Cas No.:847728-01-2
Sample solution is provided at 25 µL, 10mM.
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Ki: 3.16 nM: antagonizes E prostanoid receptor 4 (EP4).
Ki: 631 nM: antagonizes EP2.
CJ-42794, as a selective antagonist of EP4, less binds to EP2 and does not have binding affinity for EP1 or EP3. It displays minimal effect on numerous other receptors, channels, or enzymes. CJ-42794 delays the healing of gastric ulcers, inhibiting the upregulation of VEGF expression and angiogenesis. EP4, activated by prostaglandin E2 (PGE2), is a G-protein-coupled receptor, which plays vital roles in bone formation and resorption, cancer, and atherosclerosis via elevating the second messenger cyclic AMP (cAMP).
In vitro: CJ-42794 exhibited remarkable binding activity to EP4 and suppressed PGE2-triggered elevations of intracellular cAMP levels in a concentration-dependent fashion in HEK293 cells overexpressing human EP4. Moreover, CJ-42794, concentration-dependently, reversed the inhibitory effects of PGE2 on lipopolysaccharide-evoked tumor necrosis factor α production, which suggested that CJ-42794 had excellent pharmacological properties used for exploring the physiological role of EP4 [1].
In vivo: Male Sprague-Dawley rats and C57BL/6 mice were given subcutaneously 3 and 10 mg/kg for rats, 10 mg/kg for mice once daily for 7 or 14 days. Compared to the controls, CJ-42794, in a dose-dependent manner, impaired and delayed the gastric ulcer healing in rats and mice. CJ-42794 markedly dampened the increase of VEGF expression in ulcerated mucosa of the mouse stomach and the primary gastric fibroblasts of rat [2].
References:
[1]. Murase, A., Taniguchi, Y., Tonai-Kachi, H., Nakao, K., & Takada, J. In vitro pharmacological characterization of CJ-042794, a novel, potent, and selective prostaglandin EP4 receptor antagonist. Life Sciences. 2008; 82(3-4): 226-232.
[2]. Hatazawa, R., Tanaka, A., Tanigami, M., Amagase, K., Kato, S., Ashida, Y., & Takeuchi, K. Cyclooxygenase-2/prostaglandin E2 accelerates the healing of gastric ulcers via EP4 receptors. AJP: Gastrointestinal and Liver Physiology. 2007; 293(4): G788-G797.
| Cas No. | 847728-01-2 | SDF | |
| 别名 | 4-[(1S)-1-[[5-氯-2-(4-氟苯氧基)苄基]氨基]乙基]苯甲酸,RQ-00015986 | ||
| 化学名 | 4-[(1S)-1-[[5-chloro-2-(4-fluorophenoxy)benzoyl]amino]ethyl]-benzoic acid | ||
| Canonical SMILES | FC1=CC=C(OC2=C(C(N[C@@H](C)C3=CC=C(C(O)=O)C=C3)=O)C=C(Cl)C=C2)C=C1 | ||
| 分子式 | C22H17ClFNO4 | 分子量 | 413.8 |
| 溶解度 | ≥ 11.7mg/mL in DMSO | 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 | 2.4166 mL | 12.0831 mL | 24.1663 mL |
| 5 mM | 0.4833 mL | 2.4166 mL | 4.8333 mL |
| 10 mM | 0.2417 mL | 1.2083 mL | 2.4166 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet