PF-9184,1221971-47-6

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PF-9184

CAS No. : 1221971-47-6

MCE 国际站：PF-9184

产品活性：PF-9184 是一种有效且高度选择性的人微粒体前列腺素 E 合酶 1 (mPGES-1) 的抑制剂，IC₅₀ 值为 16.5 nM。PF-9184 体外抑制 IL-1β 诱导的 PGE₂ 合成。

研究领域：Immunology/Inflammation

作用靶点：PGE synthase

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.
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).

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

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