SB290157

SB290157 is a potent and selective small-molecule antagonist of the complement C3a receptor (C3aR). Originally developed by SmithKline Beecham, it functions as a competitive inhibitor that blocks the binding of the C3a anaphylatoxin to its G protein-coupled receptor, thereby preventing downstream inflammatory signaling. Preclinical studies have demonstrated its efficacy in reducing podocyte injury in diabetic nephropathy, limiting retinal edema in vein occlusion models, and attenuating neuroinflammation in tauopathy and Alzheimer's disease models. Mechanistically, SB290157 treatment has been linked to the modulation of several key pathways, including PI3K/AKT/FoxO1, Wnt/β-catenin, and p35/CDK5. While it remains a standard pharmacological tool for investigating the complement system, researchers have noted that it may exhibit partial agonist activity in certain cell types and possesses a relatively short half-life in vivo.

Other names

C3a receptor antagonistC-3a receptor antagonistC 3a receptor antagonistN2-[(2,2-diphenylethoxy)acetyl]-L-arginineSB290157 trifluoroacetateSB-290157 trifluoroacetateSB 290157 trifluoroacetate