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

EP4 receptor antagonist 1 

Cat. No.: HY-133123
Handling Instructions

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

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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].

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].

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.

2287259-07-6

SMILES

O=C(O)C1=CC=C([[email protected]@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

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

EP4 receptor antagonist 1Prostaglandin ReceptorEP4cancerimmunotherapyHEK293cellsInhibitorinhibitorinhibit

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EP4 receptor antagonist 1
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