Description
SC-560 is a member of the diaryl heterocycle class of COX inhibitors which includes celecoxib (Celebrex™) and rofecoxib (Vioxx™). However, unlike these selective COX-2 inhibitors, SC-560 is a selective inhibitor of COX-1. Using human recombinant enzymes, the IC50 value for SC-560 with respect to COX-1 is 9 nM, while the corresponding IC50 value for COX-2 is 6.3 µM.{7675} Thus, SC-560 shows 700-fold selectivity for the COX-1 enzyme. SC-560 is orally active in the rat, where 10 mg/kg completely abolishes the ionophore-induced production of TXB2 in whole blood. However, SC-560 is ineffective in the treatment of inflammation in models such as the LPS-induced rat air-pouch model, in which the COX-2 generated prostaglandins play a significant role in the inflammatory process.{1282} In whole cells, however, SC-560 appears to act as a non-selective COX inhibitor.{14472} The mechanism of the selective versus non-selective effects of SC-560 in a cell-free environment compared whole cells has not been elucidated.
Formal name: 5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazole
Synonyms:
Molecular weight: 352.7
CAS: 188817-13-2
Purity: ≥98%
Formulation: A crystalline solid
