PF-9184

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PF-9184 是一种有效的选择性 mPGES-1（微粒体前列腺素 E 合酶-1）抑制剂，IC50 为 16.5 nM。

PF-9184 is a potent, selective mPGES-1 (microsomal prostaglandin E synthase-1) inhibitor with IC50 of 16.5 nM; shows no effect against COX-1 and COX-2 (>6,500-fold selectivity); inhibits PGE2 synthesis in serum-free cell and human whole blood cultures with IC50 of 0.5-5 uM, while sparing the synthesis of PGF(1alpha)) and PGF(2alpha).

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.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.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.PF-9184 is a poor inhibitor of recombinant rat mPGES-1 (IC50=1080±398 nM).

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

PF9184

Immunology/Inflammation

PGE synthase

PGE synthase

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1221971-47-6

461.3

C21H14Cl2N2O4S

>98% (HPLC)

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

2H-1,2-Benzothiazine-3-carboxamide, N-(3',4'-dichloro[1,1'-biphenyl]-4-yl)-4-hydroxy-,1,1-dioxide

(-20℃)

With Ice Pack

≥ 2 years