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EP4 receptor antagonist 1

CAS No. : 2287259-07-6

MCE 站：EP4 receptor antagonist 1

产品活性：EP4 receptor antagonist 1 是一种高效的，竞争性的，选择性前列腺素类 EP4 受体拮抗剂。可用于癌症免疫研究。EP4 receptor antagonist 1 抑制人和小鼠 EP4 受体，IC₅₀ 分别为 6.1 nM 和 16.2 nM。对人 EP1，EP2 和 EP3 受体的 IC₅₀ >10 μM。

研究领域：GPCR/G Protein

作用靶点：Prostaglandin Receptor

In Vitro: The antagonistic effect of EP4 receptor antagonist 1 (Compounds 59) on human EP4 in calcium flux assay with an IC₅₀ of 6.1±0.2 nM in CHO-G_α16 cells overexpressing human EP4 receptor. The antagonistic effect of EP4 receptor antagonist 1 on human EP4 in calcium flux assay with an IC₅₀ of 16.2±1.7 nM in CHO-G_α16 cells overexpressing mouse EP4 receptor.
EP4 receptor antagonist 1 dose dependently inhibits PGE2-stimulated cAMP accumulation in HEK293-EP4 cells with an IC₅₀ of 18.7±0.6 nM. EP4 receptor antagonist 1 dose-dependently inhibits the activity of the CRE reporter in HEK293 cells with an IC₅₀ of 5.2±0.4 nM.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 (1 nM-10 μM) reverses PGE2-induced ERK phosphorylation in a concentration-dependent manner.

In Vivo: EP4 receptor antagonist 1 (16, 50, and 150 mg/kg; orally; once daily for two weeks) 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.
EP4 receptor antagonist 1 (1 mg/kg; intravenously) demonstrates moderate clearance (CL=1.7 L/h/kg) in mice with a corresponding favorable half-life (t_1/2) of 4.1 h. EP4 receptor antagonist 1 (5 mg/kg; orally) exhibits good bioavailability (F=48.0%) in mice with a corresponding favorable half-life (t_1/2) of 4.7 h.

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