INDOMETHACIN ESTER, N-HEPTYL-

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 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. 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.

What are the applications of Application

Indomethacin heptyl ester is a selective Cox-2 inhibitor that reduces expression and activity of MDR-1

Definition

ChEBI: Indomethacin heptyl ester is a N-acylindole.

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.