EP4 receptor antagonist 1|cas:2287259-07-6|西域试剂

EP4 receptor antagonist 1,99.0%

产品编号：Bellancom-133123| CAS NO：2287259-07-6| 分子式：C₂₃H₂₁F₃N₄O₃| 分子量：458.43

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-133123		￥9800.00	杭州北京（现货）

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EP4 receptor antagonist 1

产品介绍

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。

生物活性

EP4 receptor antagonist 1 is a highly potent and selective competitive prostanoid EP4 receptor antagonist for cancer immunotherapy. 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.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line:	CHO-EP4 cells
Concentration:	1 nM, 100 nM, 10 μM
Incubation Time:	Pretreated for 20 min and then subjected to 30 nM PGE2 simulation for 10 min.
Result:	Reversed PGE2-induced ERK phosphorylation in a concentration-dependent manner.

体内研究
(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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	BALB/c female mice (6-week-old)bearing CT26 colon cancer model
Dosage:	16, 50, and 150 mg/kg
Administration:	Orally; once daily for two weeks
Result:	Tumor growth inhibition (TGI) was 24.6% at 16 mg/ kg, 54.7% at 50 mg/kg, and 63.8% at 150 mg/kg.

Animal Model:	BALB/c female mice
Dosage:	1 mg/kg and 5 mg/kg (Pharmacokinetic Analysis)
Administration:	Intravenously or orally at a dose of 1 mg/kg (5 mL/kg) and 5 mg/kg (10 mL/kg),respectively.
Result:	Demonstrated moderate clearance ( CL=1.7 L/h/kg) in mice with a corresponding favorable half-life (t_1/2) of 4.1 h at a dose of 1 mg/kg (intravenously). Exhibited good bioavailability (F=48.0%) in mice with a corresponding favorable half-life (t_1/2) of 4.7 h at a dose of 5 mg/kg (orally).

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	BALB/c female mice (6-week-old)bearing CT26 colon cancer model
Dosage:	16, 50, and 150 mg/kg
Administration:	Orally; once daily for two weeks
Result:	Tumor growth inhibition (TGI) was 24.6% at 16 mg/ kg, 54.7% at 50 mg/kg, and 63.8% at 150 mg/kg.

Animal Model:	BALB/c female mice
Dosage:	1 mg/kg and 5 mg/kg (Pharmacokinetic Analysis)
Administration:	Intravenously or orally at a dose of 1 mg/kg (5 mL/kg) and 5 mg/kg (10 mL/kg),respectively.
Result:	Demonstrated moderate clearance ( CL=1.7 L/h/kg) in mice with a corresponding favorable half-life (t_1/2) of 4.1 h at a dose of 1 mg/kg (intravenously). Exhibited good bioavailability (F=48.0%) in mice with a corresponding favorable half-life (t_1/2) of 4.7 h at a dose of 5 mg/kg (orally).

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	BALB/c female mice (6-week-old)bearing CT26 colon cancer model
Dosage:	16, 50, and 150 mg/kg
Administration:	Orally; once daily for two weeks
Result:	Tumor growth inhibition (TGI) was 24.6% at 16 mg/ kg, 54.7% at 50 mg/kg, and 63.8% at 150 mg/kg.

Animal Model:	BALB/c female mice
Dosage:	1 mg/kg and 5 mg/kg (Pharmacokinetic Analysis)
Administration:	Intravenously or orally at a dose of 1 mg/kg (5 mL/kg) and 5 mg/kg (10 mL/kg),respectively.
Result:	Demonstrated moderate clearance ( CL=1.7 L/h/kg) in mice with a corresponding favorable half-life (t_1/2) of 4.1 h at a dose of 1 mg/kg (intravenously). Exhibited good bioavailability (F=48.0%) in mice with a corresponding favorable half-life (t_1/2) of 4.7 h at a dose of 5 mg/kg (orally).