EP4 receptor antagonist 1

SKU: orb1309698

Description

EP4 Receptor Antagonist 1 is a potent and selective competitive antagonist of the prostanoid EP4 receptor, with IC50 values of 6.1 nM (human) and 16.2 nM (mouse). It shows >1000-fold selectivity over other EP receptor subtypes. This compound is a valuable research tool for studying EP4's role in cancer immunology and inflammation in both cellular and animal models.

Research Area

Immunology & Inflammation, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2287259-07-6
• MW: 458.43
• Purity: 99.53% (May vary between batches)
• Formula: C₂₃H₂₁F₃N₄O₃
• SMILES: C\C=C\c1nnn(Cc2ccc(cc2)C(F)(F)F)c1C(=O)N[C@@H](C)c1ccc(cc1)C(O)=O
• Target: Prostaglandin Receptor

Bioactivity

• Target IC50:
  EP4 receptor (human):6.1 nM |EP4 receptor (mouse):16.2 nM
• In Vivo:
  EP4 receptor antagonist 1 (1 mg/kg; i.v.) demonstrates moderate clearance of 1.7 L/h/kg in mice with a corresponding favorable half-life of 4.1 h. EP4 receptor antagonist 1 (5 mg/kg; orally) exhibits good bioavailability of 48.0% in mice with a corresponding favorable half-life of 4.7 h. EP4 receptor antagonist 1 (16, 50, and 150 mg/kg; oral) 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.
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• In Vitro:
  EP4 receptor antagonist 1 inhibits the activity of the CRE reporter in HEK293 cells with an IC50 of 5.2±0.4 nM in a dose-dependent manner. 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. EP4 receptor antagonist 1 inhibits PGE2-stimulated cAMP accumulation in HEK293-EP4 cells with an IC50 of 18.7±0.6 nM in a dose-dependent manner. EP4 receptor antagonist 1 (1 nM-10 μM) reverses PGE2-induced ERK phosphorylation in a concentration-dependent manner. The IC50s are >10 μM for human EP1, EP2, and EP3 receptors.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

cancer, cells, Inhibitor, inhibit, immunotherapy, mouse EP4 receptor, EP4 receptor antagonist 1, EP-4 receptor antagonist 1, EP4, HEK293, human EP4 receptor, Prostaglandin Receptor, ProstaglandinReceptor

Compound Identifiers

PubChem CID

146014480