SB-657510

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SB-657510 是选择性的 urotensin II (UII) receptor (UT) 拮抗剂。 对于人，猴，猫，大鼠和小鼠的受体的 Ki 值分别为 61、17、30、65 和 56 nM。SB-657510 通过抑制 UII 诱导的人类血管内皮细胞中炎性介质，如粘附分子，细胞因子和组织因子上调发挥抗炎作用。

SB-657510 is a selective urotensin II (UII) receptor (UT) antagonist. The Ki 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.

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.SB-706375 (1-10000 nM) inhibits [Ca2+]i mobilization elicited by 10?nM hU-II with an IC50 of 180?nM.Western Blot Analysis Cell Line:EA.hy926 cells (UII-induced)Concentration:1 μM Incubation Time:0.5, 1, 2, 4, 8 hours Result:Remarkably decreased the UII-induced protein expression of tissue factor.

SB-657510 inhibits the progression of high-fat diet induced atherosclerosis and diabetes-associated atherosclerosis.Levels of phosphorylated ERK are significantly attenuated in the aorta of SB-657510-treated (30 mg/kg/day) diabetic mice (Male Apoe KO mice).

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GPCR/G Protein

Neurotensin Receptor

Neurotensin Receptor

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474960-44-6

505.81

C19H22BrClN2O5S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (197.70 mM; 超声助溶 )

COc1cc(Br)c(cc1OC)S(=O)(=O)Nc1ccc(Cl)c(O[C@@H]2CCN(C)C2)c1

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(-20℃)

With Ice Pack

≥ 2 years