EP4 receptor antagonist 1

Name: EP4 receptor antagonist 1
Brand: MedChemExpress
SKU: HY-133123
Rating: 5.0 (2 reviews)

製品番号: HY-133123 純度: 99.94%: Data Sheet SDS COA 取扱説明書
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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.

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EP4 receptor antagonist 1 構造式

CAS 番号 : 2287259-07-6

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 315	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 315	在庫あり	Estimated Time of Arrival: December 31
Solid
1 mg	$131	在庫あり	Estimated Time of Arrival: December 31
5 mg	$312	在庫あり	Estimated Time of Arrival: December 31
10 mg	$500	在庫あり	Estimated Time of Arrival: December 31
25 mg	$1000	在庫あり	Estimated Time of Arrival: December 31
50 mg	$1600	在庫あり	Estimated Time of Arrival: December 31
100 mg	$2560	在庫あり	Estimated Time of Arrival: December 31
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500 mg		お問い合わせ

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カスタマーレビュー

Based on 2 publication(s) in Google Scholar

顧客検証

Prostaglandin Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

DP EP FP IP TXA₂/TP TXB₂

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	16.2 1 Compound: 59	Antagonist activity at mouse EP4 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay Antagonist activity at mouse EP4 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay	[PMID: 31855426]
HEK293	IC₅₀	0.4 1 Compound: 59	Inhibition of human EP4 transfected in human HEK293 cells co transfected with SmBit-beta-arrestin. assessed as reduction in PGE2 induced-beta-arrestin recruitment by NanoBiT beta-arrestin recruitment assay Inhibition of human EP4 transfected in human HEK293 cells co transfected with SmBit-beta-arrestin. assessed as reduction in PGE2 induced-beta-arrestin recruitment by NanoBiT beta-arrestin recruitment assay	[PMID: 31855426]
CHO	IC₅₀	> 10000 1 Compound: 59	Antagonist activity at human EP1 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay Antagonist activity at human EP1 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay	[PMID: 31855426]
CHO	IC₅₀	6.1 1 Compound: 59	Antagonist activity at human EP4 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay Antagonist activity at human EP4 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay	[PMID: 31855426]
CHO	IC₅₀	>10 3 Compound: 59	Antagonist activity at human EP1 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay Antagonist activity at human EP1 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay	[PMID: 31855426]
CHO	IC₅₀	> 10000 1 Compound: 59	Antagonist activity at human EP2 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay Antagonist activity at human EP2 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay	[PMID: 31855426]
CHO	IC₅₀	> 10000 1 Compound: 59	Antagonist activity at human EP1 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay Antagonist activity at human EP1 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay	[PMID: 31855426]
HEK293	IC₅₀	5.2 1 Compound: 59	Inhibition of human EP4 transfected in human HEK293 cells co transfected with CRE-luciferase assessed as reduction in PGE2-induced luciferase expression incubated for 24 hrs by luciferase reporter gene Assay Inhibition of human EP4 transfected in human HEK293 cells co transfected with CRE-luciferase assessed as reduction in PGE2-induced luciferase expression incubated for 24 hrs by luciferase reporter gene Assay	[PMID: 31855426]
CHO	IC₅₀	> 10000 1 Compound: 59	Antagonist activity at human EP3 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay Antagonist activity at human EP3 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay	[PMID: 31855426]
CHO	IC₅₀	> 10000 1 Compound: 59	Antagonist activity at human EP2 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay Antagonist activity at human EP2 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay	[PMID: 31855426]
CHO	IC₅₀	6.1 1 Compound: 59	Antagonist activity at human EP4 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay Antagonist activity at human EP4 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay	[PMID: 31855426]
CHO	IC₅₀	16.2 1 Compound: 59	Antagonist activity at mouse EP4 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay Antagonist activity at mouse EP4 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay	[PMID: 31855426]
CHO	IC₅₀	> 10000 1 Compound: 59	Antagonist activity at human EP3 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay Antagonist activity at human EP3 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay	[PMID: 31855426]
CHO	IC₅₀	16.2 1 Compound: 59	Antagonist activity at mouse EP4 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay Antagonist activity at mouse EP4 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay	[PMID: 31855426]
CHO	IC₅₀	6.1 1 Compound: 59	Antagonist activity at human EP4 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay Antagonist activity at human EP4 expressed in CHO cells coexpressing G16-alpha assessed as intracellular calcium flux preincubated for 15 mins followed by addition of PGE2 by calcium flux assay	[PMID: 31855426]
HEK293	IC₅₀	18.7 1 Compound: 59	Inhibition of human EP4 transfected in human HEK293 cells assessed as reduction in PGE2-induced cAMP level incubated for 15 mins followed by PGE2 stimulation and measured every 2 mins for 30 mins by GloSensor cAMP Assay Inhibition of human EP4 transfected in human HEK293 cells assessed as reduction in PGE2-induced cAMP level incubated for 15 mins followed by PGE2 stimulation and measured every 2 mins for 30 mins by GloSensor cAMP Assay	[PMID: 31855426]
HEK293	IC₅₀	0.4 1 Compound: 59	Inhibition of human EP4 transfected in human HEK293 cells co transfected with SmBit-beta-arrestin. assessed as reduction in PGE2 induced-beta-arrestin recruitment by NanoBiT beta-arrestin recruitment assay Inhibition of human EP4 transfected in human HEK293 cells co transfected with SmBit-beta-arrestin. assessed as reduction in PGE2 induced-beta-arrestin recruitment by NanoBiT beta-arrestin recruitment assay	[PMID: 31855426]
HEK293	IC₅₀	18.7 1 Compound: 59	Inhibition of human EP4 transfected in human HEK293 cells assessed as reduction in PGE2-induced cAMP level incubated for 15 mins followed by PGE2 stimulation and measured every 2 mins for 30 mins by GloSensor cAMP Assay Inhibition of human EP4 transfected in human HEK293 cells assessed as reduction in PGE2-induced cAMP level incubated for 15 mins followed by PGE2 stimulation and measured every 2 mins for 30 mins by GloSensor cAMP Assay	[PMID: 31855426]
HEK293	IC₅₀	5.2 1 Compound: 59	Inhibition of human EP4 transfected in human HEK293 cells co transfected with CRE-luciferase assessed as reduction in PGE2-induced luciferase expression incubated for 24 hrs by luciferase reporter gene Assay Inhibition of human EP4 transfected in human HEK293 cells co transfected with CRE-luciferase assessed as reduction in PGE2-induced luciferase expression incubated for 24 hrs by luciferase reporter gene Assay	[PMID: 31855426]
HEK293	IC₅₀	0.4 1 Compound: 59	Inhibition of human EP4 transfected in human HEK293 cells co transfected with SmBit-beta-arrestin. assessed as reduction in PGE2 induced-beta-arrestin recruitment by NanoBiT beta-arrestin recruitment assay Inhibition of human EP4 transfected in human HEK293 cells co transfected with SmBit-beta-arrestin. assessed as reduction in PGE2 induced-beta-arrestin recruitment by NanoBiT beta-arrestin recruitment assay	[PMID: 31855426]
HEK293	IC₅₀	18.7 1 Compound: 59	Inhibition of human EP4 transfected in human HEK293 cells assessed as reduction in PGE2-induced cAMP level incubated for 15 mins followed by PGE2 stimulation and measured every 2 mins for 30 mins by GloSensor cAMP Assay Inhibition of human EP4 transfected in human HEK293 cells assessed as reduction in PGE2-induced cAMP level incubated for 15 mins followed by PGE2 stimulation and measured every 2 mins for 30 mins by GloSensor cAMP Assay	[PMID: 31855426]
HEK293	IC₅₀	5.2 1 Compound: 59	Inhibition of human EP4 transfected in human HEK293 cells co transfected with CRE-luciferase assessed as reduction in PGE2-induced luciferase expression incubated for 24 hrs by luciferase reporter gene Assay Inhibition of human EP4 transfected in human HEK293 cells co transfected with CRE-luciferase assessed as reduction in PGE2-induced luciferase expression incubated for 24 hrs by luciferase reporter gene Assay	[PMID: 31855426]

体外実験

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^[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].

MedChemExpress (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.

体内実験

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 (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^[1].

MedChemExpress (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 (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).

分子量

458.43

分子式

C₂₃H₂₁F₃N₄O₃

CAS 番号

2287259-07-6

Appearance

Solid

Color

White to off-white

SMILES

O=C(O)C1=CC=C([C@@H](NC(C2=C(/C=C/C)N=NN2CC3=CC=C(C(F)(F)F)C=C3)=O)C)C=C1

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : 100 mg/mL (218.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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
10 mM	0.2181 mL	1.0907 mL	2.1814 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator

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純度とドキュメンテーション

純度: 99.94%

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データシート (282 KB) SDS (251 KB)

COA (255 KB) HNMR (442 KB) RP-HPLC (258 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Yang JJ, et al. Discovery and Characterization of 1H-1,2,3-Triazole Derivatives as Novel Prostanoid EP4 Receptor Antagonists for Cancer Immunotherapy. J Med Chem. 2020 Jan 23;63(2):569-590. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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