A potent inhibitor of mPGES-1 (IC50 = 16.5 nM for recombinant human enzyme); blocks the synthesis of PGE2 in LPS-treated human whole blood and in IL-1β-stimulated fibroblasts (IC50s = 0.4-5 µM)

PF-9184 – 10 mg

Brand:
Cayman
CAS:
1221971-47-6
Storage:
-20
UN-No:
Non-Hazardous - /

Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product prostaglandin H2 (PGH2; Item No. 17020) into the biologically active PGE2 (Item No. 14010).{7229} Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1β, and TNF-α.{11537} PF-9184 is a potent inhibitor of mPGES-1 (IC50 = 16.5 nM for recombinant human enzyme).{30680} It displays at least 6,500-fold selectivity for mPGES-1 over COX-1 and COX-2. PF-9184 blocks the synthesis of PGE2 in LPS-treated human whole blood and in IL-1β-stimulated fibroblasts (IC50s = 0.4-5 µM).{30723,30679}  

 

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Description

A potent inhibitor of mPGES-1 (IC50 = 16.5 nM for recombinant human enzyme); blocks the synthesis of PGE2 in LPS-treated human whole blood and in IL-1β-stimulated fibroblasts (IC50s = 0.4-5 µM)

Formal name: N-​(3′,​4′-​dichloro[1,​1′-​​biphenyl]​-​4-​​yl)​-​4-​​hydroxy-​2H-​1,​2-​​benzothiazine-​​3-​carboxamide 1,​1-​​dioxide

Synonyms: 

Molecular weight: 461.3

CAS: 1221971-47-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Prostaglandin Synthases||Research Area|Immunology & Inflammation|Inflammatory Lipid Mediators|Prostaglandins||Research Area|Lipid Biochemistry|Cyclooxygenase Pathway

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