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PF-9184

PF-9184
PF-9184 is a potent and selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1) with an IC50 of 16.5 nM, and it inhibits IL-1β-induced PGE2 synthesis in vitro.
Catalog No. T21738Cas No. 1221971-47-6
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Purity:97.64%
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PF-9184

Catalog No. T21738Cas No. 1221971-47-6
PF-9184 is a potent and selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1) with an IC50 of 16.5 nM, and it inhibits IL-1β-induced PGE2 synthesis in vitro.
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1 mg$30In Stock
5 mg$69In Stock
10 mg$105In Stock
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Product Introduction

Bioactivity
Description
PF-9184 is a potent and selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1) with an IC50 of 16.5 nM, and it inhibits IL-1β-induced PGE2 synthesis in vitro.
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)[1].
In vivo
PF-9184, whether administered orally or locally, does not affect PGE2 synthesis in recombinant rats[1].
Chemical Properties
Molecular Weight461.32
FormulaC21H14Cl2N2O4S
Cas No.1221971-47-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 60 mg/mL (130.06 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1677 mL10.8385 mL21.6769 mL108.3846 mL
5 mM0.4335 mL2.1677 mL4.3354 mL21.6769 mL
10 mM0.2168 mL1.0838 mL2.1677 mL10.8385 mL
20 mM0.1084 mL0.5419 mL1.0838 mL5.4192 mL
50 mM0.0434 mL0.2168 mL0.4335 mL2.1677 mL
100 mM0.0217 mL0.1084 mL0.2168 mL1.0838 mL

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