| Description | SB-657510 is a urotensin II (UII) receptor (UT) antagonist. The Ki values of UT for human, monkey, cat, rat and mouse were 61, 17, 30, 65 and 56 nM, respectively. SB-657510 plays an anti-inflammatory role by inhibiting UII-induced inflammatory mediators, such as adhesion molecules, in human vascular endothelial cells and upregulation of cytokines and tissue factors. SB 657510 has a therapeutic effect on diabetes-related atherosclerotic disease in diabetic mouse models. |
| In vitro | UII诱导的U937和EA.hy926细胞间的粘附增加，被SB-657510显著阻断。SB-657510（1 μM；0.5-8小时）阻止UII在内皮细胞中诱导的组织因子表达。[1] SB-706375（1-10000 nM）抑制10 nM hU-II引起的[Ca2+]i释放（IC50为180 nM）。[2] |
| In vivo | SB-657510显著抑制了由高脂饮食引起的动脉粥样硬化以及糖尿病相关动脉粥样硬化的进展。[1] 在接受SB-657510处理的糖尿病小鼠（雄性Apoe KO小鼠；剂量为30 mg/kg/day）的主动脉中，磷酸化ERK的水平显著降低。[3] |
| Target activity | UTII receptor (human):61 nM, UTII receptor (monkey):17 nM, UTII receptor (cat):30 nM, UTII receptor (rat):65 nM, UTII receptor (mouse):56 nM |
| molecular weight | 505.81 |
| Molecular formula | C19H22BrClN2O5S |
| CAS | 474960-44-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 27.0 mg/mL (53.4 mM) |
| References | 1. Park SL, et al. Inhibitory Effect of an Urotensin II Receptor Antagonist on Proinflammatory Activation Inducedby Urotensin II in Human Vascular Endothelial Cells. Biomol Ther (Seoul). 2013;21(4):277-283. 2. Behm DJ, et al. Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues. Br J Pharmacol. 2008;155(3):374-386. 3. Watson AM, et al. Urotensin II receptor antagonism confers vasoprotective effects in diabetes associated atherosclerosis: studies in humans and in a mouse model of diabetes. Diabetologia. 2013;56(5):1155-1165. |