Indomethacin heptyl ester

Indomethacin is a potent but non-selective inhibitor of both COX-1 and COX-2 in sheep and humans.¹ 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 IC₅₀ 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-1.² While indomethacin itself has an IC₅₀ of 0.05 µM for the inhibition of COX-2, it also inhibits COX-1 with a corresponding IC₅₀ of 0.67 µM.²

WARNING This product is not for human or veterinary use.

1. Barnett, J., Chow, J., Ives, D., et al. Purification, characterization and selective inhibition of human prostaglandin G/H synthase 1 and 2 expressed in the baculovirus system. Biochim. Biophys. Acta 1209(1), 130-139 (1994).

2. Kalgutkar, A.S., Marnett, A.B., Crews, B.C., et al. Ester and amide derivatives of the nonsteroidal antiinflammatory drug, indomethacin, as selective cyclooxygenase-2 inhibitors. J. Med. Chem. 43(15), 2860-2870 (2000).