1. Immunology/Inflammation
  2. PGE synthase
  3. PF-9184

PF-9184 

Cat. No.: HY-19622
Handling Instructions

PF-9184 is a potent and highly selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1), with an IC50 of 16.5 nM. PF-9184 inhibits IL-1β-induced PGE2 synthesis in vitro.

For research use only. We do not sell to patients.

PF-9184 Chemical Structure

PF-9184 Chemical Structure

CAS No. : 1221971-47-6

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Description

PF-9184 is a potent and highly selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1), with an IC50 of 16.5 nM. PF-9184 inhibits IL-1β-induced PGE2 synthesis in vitro[1].

IC50 & Target

IC50: 16.5 nM (mPGES-1)[1]

In Vitro

PF-9184 (0.015-100 μM; 24 hours) inhibits IL-1β-stimulated prostaglandin E2 (PGE2) synthesis in rheumatoid arthritis (RASF) in synovial fibroblasts derived from patients and has no apparent cytotoxic effects up to 100 μM[1].
PF-9184 (0.015-100 μM) potently blocks mPGES-1 ability to synthesize PGE2 from PGH2, and with no apparent inhibitory effects on COX-2 and prostacyclin synthase in cells[1].
PF-9184 (0.015-100 μM) inhibits PGE2 weakly but has no effect on TXB2 synthesis except at 100 μM in human whole blood and modified blood assays[1].
PF-9184 is a poor inhibitor of recombinant rat mPGES-1 (IC50=1080±398 nM)[1].

In Vivo

PF-9184 (oral administration or even local delivery) has no effect on PGE2 synthesis in recombinant rats[1].

Molecular Weight

461.32

Formula

C₂₁H₁₄Cl₂N₂O₄S

CAS No.

1221971-47-6

SMILES

O=C(C1=C(O)C2=CC=CC=C2S(N1)(=O)=O)NC3=CC=C(C4=CC=C(Cl)C(Cl)=C4)C=C3

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:

PF-9184PF9184PF 9184PGE synthaseProstaglandin E synthasemicrosomalprostaglandinsynthase-1mPGES-1inflammationosteoarthritisrheumatoidarthritisInhibitorinhibitorinhibit

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PF-9184
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HY-19622
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