Zaloglanstat

Description

Zaloglanstat ISC-27864; GRC-27864 is a selective, orally active microsomal mPGES-1 inhibitor. Zaloglanstat has an IC50 of 5 nM for human mPGES-1 without significant inhibitory effect on COX-1/2 IC50 10 ?M. Zaloglanstat blocks the conversion of arachidonic acid metabolite prostaglandin PGH2 to prostaglandin PGE2, thereby inhibiting inflammation-related PGE2 overproduction and reducing inflammatory responses and pain. Zaloglanstat inhibits IL-1?-induced PGE2 release in A549 cells and human synovial fibroblasts in vitro. Zaloglanstat inhibits PGE2 release in pig and dog whole blood with IC50s ??of 161 nM and 154 nM, respectively. Zaloglanstat can be used in the study of asthma, osteoarthritis, and neurodegenerative diseases.