gw-274150

Description: GW-274150 is a novel, potent, arginine-competitive, highly selective, NADPH-dependent, and long-acting inhibitor of inducible nitric oxide synthase (iNOS) activity in rat and mouse models of renal I/R. GW274150 was identified from a series of acetamide amino acids that have a high selectivity for iNOS vs both eNOS (> 260-fold) and nNOS (> 219-fold) and high bioavailability (> 90%) after oral administration. GW274150 reduced histologic evidence of tubular injury and markedly reduced immunohistochemical evidence of nitrotyrosine and PAR formation, indicating reduced peroxynitrite formation and poly (ADP-ribose) polymerase (PARP) activation, respectively. It may be helpful in treating renal dysfunction and injury associated with I/R of the kidney.

References: Free Radic Biol Med. 2011 Mar 1; 50(5):633-40.; Clin Exp Rheumatol. 2012 Mar-Apr; 30(2):254-61.