PF-04418948

SKU: orb1227026

Description

PF-04418948 (PF 04418948) is a novel potent and selective prostaglandin EP2 receptor antagonist; inhibits prostaglandin E(2)(PGE(2))-induced increase in cAMP in cells with a functional K(B) value of 1.8 nM; attenuates the butaprost-induced cutaneous blood flow response in rats; orally active.(In Vitro):PF-04418948 (2 μM; 90 min) inhibits prostaglandin E2 (PGE2)-induced increase in cAMP.(In Vivo):PF-04418948 (oral gavage; 1, 3, and 10 mg/kg; once) attenuats the butaprost-induced cutaneous blood flow response.

Key Properties

• CAS Number: 1078166-57-0
• MW: 409.407
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₀FNO₅
• SMILES: COC1=CC2=C(C=C1)C=C(C=C2)OCC3(CN(C3)C(=O)C4=CC=C(C=C4)F)C(=O)O
• Target: Prostaglandin Receptor
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  PF-04418948 (oral gavage; 1, 3, and 10 mg/kg; once) attenuats the butaprost-induced cutaneous blood flow response. Animal model: Sprague Dawley rats. Dosage: 1, 3, and 10 mg/kg. Administration: Oral gavage; 1, 3, and 10 mg/kg; once. Result: Reduced the peak and AUC butaprost-induced cutaneous blood flow response in a dose-dependent fashion.
• In Vitro:
  PF-04418948 (2 μM; 90 min) inhibits prostaglandin E2 (PGE2)-induced increase in cAMP. Cell Viability Assay Cell line: CHO cells. Concentration: 2 μM. Incubation time: 90 min. Result: Inhibited prostaglandin E2 (PGE2)-induced increase in cAMP in cells expressing EP2 receptors with a functional KB value of 1.8 nM.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Prostaglandin Receptor