Powder: -20°C for 3 years | In solvent: -80°C for 1 year
EP4 receptor antagonist 1 是一种有效的特异性前列腺素 EP4受体拮抗剂,对人和小鼠 EP4受体的 IC50分别为6.1 nM 和16.2 nM。 EP4 receptor antagonist 1 可用于癌症免疫治疗的研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 847 | 现货 | ||
5 mg | ¥ 2,370 | 现货 | ||
10 mg | ¥ 3,530 | 现货 | ||
25 mg | 待询 | 现货 | ||
50 mg | 待询 | 现货 |
产品描述 | EP4 Receptor Antagonist 1 is a highly potent and selective competitive prostanoid EP4 receptor antagonist, effective for cancer immunotherapy. It inhibits both human and mouse EP4 receptors with IC50 values of 6.1 nM and 16.2 nM, respectively, while displaying minimal activity (IC50s >10 μM) against human EP1, EP2, and EP3 receptors. |
靶点活性 | EP4 receptor (human):6.1 nM , EP4 receptor (mouse):16.2 nM |
体外活性 | EP4 receptor antagonist 1 inhibits the activity of the CRE reporter in HEK293 cells with an IC50 of 5.2±0.4 nM in a dose-dependent manner. EP4 receptor antagonist 1 dose-dependently inhibits PGE2-stimulated β-arrestin recruitment in HEK293-EP4 cells with an IC50 of 0.4±0.1 nM. EP4 receptor antagonist 1 inhibits PGE2-stimulated cAMP accumulation in HEK293-EP4 cells with an IC50 of 18.7±0.6 nM in a dose-dependent manner. EP4 receptor antagonist 1 (1 nM-10 μM) reverses PGE2-induced ERK phosphorylation in a concentration-dependent manner. The IC50s are >10 μM for human EP1, EP2, and EP3 receptors[1]. |
体内活性 | EP4 receptor antagonist 1 (1 mg/kg; i.v.) demonstrates moderate clearance of 1.7 L/h/kg in mice with a corresponding favorable half-life of 4.1 h. EP4 receptor antagonist 1 (5 mg/kg; orally) exhibits good bioavailability of 48.0% in mice with a corresponding favorable half-life of 4.7 h. EP4 receptor antagonist 1 (16, 50, and 150 mg/kg; oral) causes significant inhibition of tumor growth in BALB/c female mice. No significant body weight loss is found in any mouse cohorts. EP4 receptor antagonist 1 is well tolerated in mice at the tested dosage[1]. |
分子量 | 458.43 |
分子式 | C23H21F3N4O3 |
CAS No. | 2287259-07-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
EP4 receptor antagonist 1 2287259-07-6 GPCR/G Protein Immunology/Inflammation Prostaglandin Receptor HEK293 EP4 immunotherapy Inhibitor inhibit EP-4 receptor antagonist 1 cells cancer inhibitor