EP4 receptor antagonist 1

EP4 receptor antagonist 1，Cas号 2287259-07-6，纯度: 99.53%，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。更多视频请关注视频号【艾维缔】。哔哩哔哩【IVDSHOW】。抖音【军哥聊表观】。

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所属分类

抑制剂

目录号

T11211

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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。

生物活性

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(IC₅₀)	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].

化学信息

分子量	458.43
分子式	C₂₃H₂₁F₃N₄O₃
CAS No.	2287259-07-6
Smiles	C\C=C\c1nnn(Cc2ccc(cc2)C(F)(F)F)c1C(=O)N[C@@H](C)c1ccc(cc1)C(O)=O
密度	1.32 g/cm3 (Predicted)

产品组分

内容	型号	规格	储存温度
EP4 receptor antagonist 1	T11211-01	1mg	-20°C
EP4 receptor antagonist 1	T11211-02	5mg	-20°C
EP4 receptor antagonist 1	T11211-03	10mg	-20°C
EP4 receptor antagonist 1	T11211-04	25mg	-20°C
操作手册	1	1	常温

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FAQ
1.Mdluli K, et al. Science, 1998, 280(5369), 1607-1610.

2.Slayden RA, et al. Mol Microbiol, 2000, 38(3), 514-525.

3.Timmins GS, et al. Mol Microbiol, 2006, 62(5), 1220-1227.

4.Nicod L, et al. Hum Exp Toxicol, 1997, 16(1), 28-34.

5.Poloyac SM, et al. Drug Metab Dispos, 2004, 32(7), 727-733.

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Pharmacological research | 2025 Apr 16 | 40250509