GW274150

GW274150 is a potent, selective, orally active small molecule inhibitor of human inducible nitric oxide synthase (iNOS; also known as NOS2). It acts as an NADPH-dependent and arginine-competitive inhibitor with high selectivity for iNOS over endothelial NOS (eNOS) and neuronal NOS (nNOS), showing more than 100-fold selectivity against eNOS and over 80-fold against nNOS. The compound was developed by GlaxoSmithKline for potential anti-inflammatory activity in conditions such as migraine and rheumatoid arthritis. Clinical trials reached up to phase II for rheumatoid arthritis and migraine disorders, and phase I for mild asthma; however, all clinical development was discontinued. Mechanistically, by inhibiting iNOS-mediated nitric oxide production—a key mediator in inflammation—GW274150 aimed to reduce inflammatory responses implicated in pain conditions with an inflammatory component[1][3][4][6].

Other names

L-Homocysteine, S-(2-((1-iminoethyl)amino)ethyl)