1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. EP4 receptor antagonist 1

EP4 receptor antagonist 1 

目录号: HY-133123 纯度: 99.66%
COA 产品使用指南

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。

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EP4 receptor antagonist 1 Chemical Structure

EP4 receptor antagonist 1 Chemical Structure

CAS No. : 2287259-07-6

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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1].

IC50 & Target

IC50: 6.1 nM (human EP4 receptor), 16.2 nM (mouse EP4 receptor)[1]

体外研究
(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-Gα16 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-Gα16 cells overexpressing mouse EP4 receptor[1].
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[1].
EP4 receptor antagonist 1 (1 nM-10 μM) reverses PGE2-induced ERK phosphorylation in a concentration-dependent manner[1].

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

Western Blot Analysis[1]

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[1].
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 (t1/2) 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 (t1/2) of 4.7 h[1].

MCE 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[1]
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[1]
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 (t1/2) 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 (t1/2) of 4.7 h at a dose of 5 mg/kg (orally).
分子量

458.43

Formula

C23H21F3N4O3

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (218.14 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1814 mL 10.9068 mL 21.8136 mL
5 mM 0.4363 mL 2.1814 mL 4.3627 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.66%

参考文献

EP4 receptor antagonist 1 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1814 mL 10.9068 mL 21.8136 mL 54.5340 mL
5 mM 0.4363 mL 2.1814 mL 4.3627 mL 10.9068 mL
10 mM 0.2181 mL 1.0907 mL 2.1814 mL 5.4534 mL
15 mM 0.1454 mL 0.7271 mL 1.4542 mL 3.6356 mL
20 mM 0.1091 mL 0.5453 mL 1.0907 mL 2.7267 mL
25 mM 0.0873 mL 0.4363 mL 0.8725 mL 2.1814 mL
30 mM 0.0727 mL 0.3636 mL 0.7271 mL 1.8178 mL
40 mM 0.0545 mL 0.2727 mL 0.5453 mL 1.3633 mL
50 mM 0.0436 mL 0.2181 mL 0.4363 mL 1.0907 mL
60 mM 0.0364 mL 0.1818 mL 0.3636 mL 0.9089 mL
80 mM 0.0273 mL 0.1363 mL 0.2727 mL 0.6817 mL
100 mM 0.0218 mL 0.1091 mL 0.2181 mL 0.5453 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
EP4 receptor antagonist 1
目录号:
HY-133123
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