Cat. No.: HY-133123

EP4 receptor antagonist 1

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

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.

For research use only. We do not sell to patients.

Purity: 99.94%
CAS No.: 2287259-07-6
Formula: C₂₃H₂₁F₃N₄O₃
Molecular Weight:458.43

Storage:

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

EP4 receptor antagonist 1 Chemical Structure

CAS No.: 2287259-07-6

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

All Prostaglandin Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	>10000 nM 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 nM 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 nM 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 nM 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	>10000 nM 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	0.4 nM 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 nM 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 nM 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]

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^[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.

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 (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).

Chemical Information

CAS No. 2287259-07-6
Appearance Solid
Molecular Weight 458.43
Formula C₂₃H₂₁F₃N₄O₃
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
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Publications (2)

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Journal Impact Factor

Cell

Systemic immune activity occurs during human immune system maturation. [Abstract]

2025 Dec 11;188(25):7291-7308.e23. PMID: 41161316
J Lipid Res

EBV promotes alveolar trabecula resorption via extracellular vesicle remodeling by group IIA secreted phospholipase A2. [Abstract]

2026 Mar 3;67(4):101014. PMID: 41786250

Solvent & Solubility

In Vitro:

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)

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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

Keywords

EP4 receptor antagonist 1

2 Cited Publications

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EP4 receptor antagonist 1

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Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

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Publications Citing Use of MedChemExpress (MCE) EP4 receptor antagonist 1

All Prostaglandin Receptor Isoforms

Biological Activity

Chemical Information

Publications (2)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

EP4 receptor antagonist 1

Bioactive Compound Library Max

Bioactive Compound Library

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Angiogenesis-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

MCE Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) EP4 receptor antagonist 1

All Prostaglandin Receptor Isoforms

Biological Activity

Chemical Information

Publications (2)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

EP4 receptor antagonist 1 Related Classifications

HY-133123 Related Classifications