SB-657510

SB-657510 is a selective urotensin II (UII) receptor (UT) antagonist. The K_i values are 61, 17, 30, 65 and 56 nM for human, monkey, cat, rat and mouse receptors, respectively. SB-657510 exerts anti-inflammatory effects by inhibiting UII-induced upregulation of inflammatory mediators such as adhesion molecules, cytokines, and tissue factor in human vascular endothelial cells^[1][2]. In Vitro: SB-657510 dramatically blocks the UII-induced increase in adhesion between U937 and EA.hy926 cell. SB-657510 (1 μM; 0.5-8 hours) blocks the expression of tissue factor induced by UII in endothelial cells^[1].
SB-706375 (1-10000 nM) inhibits [Ca²⁺]_i mobilization elicited by 10?nM hU-II with an IC₅₀ of 180?nM^[2]. In Vivo: SB-657510 inhibits the progression of high-fat diet induced atherosclerosis and diabetes-associated atherosclerosis^[1].
Levels of phosphorylated ERK are significantly attenuated in the aorta of SB-657510-treated (30 mg/kg/day) diabetic mice (Male Apoe KO mice)^[3].