DUP-697

DUP-697 화학적 특성, 용도, 생산

• 개요

  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 IC₅₀ values for human recombinant COX-2 are 80 and 40 nM at 5 and 10 minutes, respectively. The IC₅₀ 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.

• 용도

  DuP-697 is a thiophene that inhibits COX-2 and acts as a NSAID.

• 생물학적 활성

  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.

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