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EP4 Receptor Antagonist 1
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产品介绍
产品介绍
产品信息
抗原名称
human EP4 receptor:6.1 nM, mouse EP4 receptor:16.2 nM
商品描述
EP4 receptor antagonist 1 inhibits human and mouse EP4 receptor with IC50s of 6.1 nM and 16.2 nM, respectively. IC50s >10 μM for human EP1, EP2,and EP3 receptors.EP4 receptor antagonist 1 is a highly potent and selective competitive prostanoid EP4 receptor antagonist for cancer immunotherapy.
纯度
98%
In vitro(体外研究)
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].
In vivo(体内研究)
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].
背景
分子式
C23H21F3N4O3
CAS号
2287259-07-6
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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