产品
编 号：F080815
分子式：C21H14Cl2N2O4S
分子量：461.32
分子式：C21H14Cl2N2O4S
分子量：461.32
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CAS No: 1221971-47-6
产品详情
生物活性：
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.
体内研究：
PF-9184 (oral administration or even local delivery) has no effect on PGE2 synthesis in recombinant rats.
体外研究：
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 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.
体内研究：
PF-9184 (oral administration or even local delivery) has no effect on PGE2 synthesis in recombinant rats.
体外研究：
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).
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