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

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.

EP4 receptor antagonist 1 Chemical Structure

EP4 receptor antagonist 1 Chemical Structure

CAS No. : 2287259-07-6

Size Price Stock Quantity
1 mg USD 426 In-stock
5 mg USD 980 In-stock
10 mg   Get quote  
50 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

EP4 receptor antagonist 1 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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]
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].

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

EP4 receptor antagonist 1 Related Antibodies

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 (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].

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 (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).
Molecular Weight

458.43

Formula

C23H21F3N4O3
CAS No.
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
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
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)

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
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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.66%

COA (255 KB) HNMR (442 KB) RP-HPLC (393 KB)

Handling Instructions (2659 KB)
References

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.

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

EP4 receptor antagonist 1 Related Classifications

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.

Keywords:

EP4 receptor antagonist 12287259-07-6Prostaglandin ReceptorEP4cancerimmunotherapyHEK293cellsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
EP4 receptor antagonist 1
Cat. No.:
HY-133123
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.