2-(4-フルオロフェニル)-3-[4-(メチルスルホニル)フェニル]-5-ブロモチオフェン 化学特性,用途語,生産方法
説明
DuP-
697 is a member of the diaryl heterocycle group of selective COX-
2 inhibitors which includes MK-
966 (rofecoxib), SC-
58125, and celecoxib. DuP-
697 is a potent and time-
dependent inhibitor of COX-
2. When tested on isolated recombinant enzymes, DuP-
697 is at least 50 times more potent in the inhibition of COX-
2 than COX-
1. The IC
50 values for human recombinant COX-
2 are 80 and 40 nM at 5 and 10 minutes, respectively. The IC
50 for the inhibition of human recombinant COX-
1 after the same time intervals is 9 μM. DuP-
697 also attenuates the COX-
1 inhibitory activity of non-
selective COX inhibitors such as indomethacin.
使用
DuP-697 is a thiophene that inhibits COX-2 and acts as a NSAID.
生物活性
Potent and selective inhibitor of cyclooxygenase-2 (IC 50 values are 10 and 800 nM for COX-2 and COX-1 respectively). Inhibits prostaglandin synthesis and is anti-inflammatory in vivo . Orally active.
2-(4-フルオロフェニル)-3-[4-(メチルスルホニル)フェニル]-5-ブロモチオフェン 上流と下流の製品情報
原材料
準備製品