DuP-697

DuP-697是选择性COX-2抑制剂二芳基杂环组的成员，该抑制剂包括MK-966（罗非昔布）、SC-58125和塞来昔布。DuP-697是一种强效且时间依赖性的COX-2抑制剂。在分离的重组酶上进行测试时，DuP-697对COX-2的抑制作用至少比对COX-1的抑制作用强50倍。人类重组COX-2的IC50值在5分钟和10分钟时分别为80和40nM。人类重组COX-1在相同时间间隔后的抑制IC50为9µM。DuP-697还会减弱非选择性COX抑制剂（如吲哚美辛）对COX-1的抑制活性。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.分子式C17H12BrFO2S2分子量411.3Fc1ccc(cc1)c1sc(Br)cc1c1ccc(cc1)S(=O)(=O)C