PF-9184_product_DataBase

Bioactivity	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[1].
Target	IC50: 16.5 nM (mPGES-1)
Invitro	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[1].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[1].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[1].PF-9184 is a poor inhibitor of recombinant rat mPGES-1 (IC50=1080±398 nM)[1].
In Vivo	PF-9184 (oral administration or even local delivery) has no effect on PGE2 synthesis in recombinant rats[1].
Name	PF-9184
CAS	1221971-47-6
Formula	C21H14Cl2N2O4S
Molar Mass	461.32
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Gabriel M, et, al. Distinction of microsomal prostaglandin E synthase-1 (mPGES-1) inhibition from cyclooxygenase-2 inhibition in cells using a novel, selective mPGES-1 inhibitor. Biochem Pharmacol. 2010 May 15; 79(10): 1445-54.

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