PF-9184

SKU: orb1704983

Description

PF-9184 is a potent and selective small molecule inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1) with an IC50 of 16.5 nM. It effectively blocks IL-1β-induced PGE2 production in vitro and is a valuable research tool for studying inflammation, pain, and cancer pathways in cellular models.

Research Area

Immunology & Inflammation, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1221971-47-6
• MW: 461.32
• Purity: 97.64% (May vary between batches)
• Formula: C₂₁H₁₄Cl₂N₂O₄S
• SMILES: OC1=C(NS(=O)(=O)c2ccccc12)C(=O)Nc1ccc(cc1)-c1ccc(Cl)c(Cl)c1
• Target: Prostaglandin Receptor,PGE Synthase
• Solubility: DMSO:60 mg/mL (130.06 mM)

Bioactivity

• In Vivo:
  PF-9184, whether administered orally or locally, does not affect PGE2 synthesis in recombinant rats.
• In Vitro:
  PF-9184 (0.015-100 μM; 24 hours) inhibits IL-1β-stimulated prostaglandin E2 (PGE2) synthesis in synovial fibroblasts derived from rheumatoid arthritis (RASF) patients with no apparent cytotoxic effects. It potently blocks mPGES-1's ability to synthesize PGE2 from PGH2 without inhibiting COX-2 and prostacyclin synthase in cells. In human whole blood and modified blood assays, PF-9184 weakly inhibits PGE2 and affects TXB2 synthesis only at 100 μM. PF-9184 poorly inhibits recombinant rat mPGES-1 (IC50=1080±398 nM).
  Read more...

Storage & Handling

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

Alternative Names

mPGES-1, ProstaglandinReceptor, Prostaglandin Receptor, PF-9184, PF9184, PF 9184

Compound Identifiers

PubChem CID

54728414