Description
Indomethacin is a potent but non-
selective inhibitor of both COX-
1 and COX-
2 in sheep and humans. Structurally, indomethacin is a substituted indole acetic acid, wherein the carboxylate can be derivatized as an ester or amide. These derivatives show enhanced selectivity for the COX-
2 isoform. For example, the IC
50 for indomethacin heptyl ester for the inhibition of human recombinant COX-
2 is 0.04 μM, making it more than 1,700 times more potent as an inhibitor of COX-
2 than COX-
1. While indomethacin itself has an IC
50 of 0.05 μM for the inhibition of COX-
2, it also inhibits COX-
1 with a corresponding IC
50 of 0.67 μM.
References
[1]. kalgutkar as, marnett ab, crews bc, et al. ester and amide derivatives of the nonsteroidal antiinflammatory drug, indomethacin, as selective cyclooxygenase-2 inhibitors. j med chem. 2000 jul 27;43(15):2860-70.
