您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > SB-657510
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
SB-657510
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SB-657510图片
CAS NO:474960-44-6
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
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。
生物活性

SB-657510 is a selectiveurotensin II (UII) receptor (UT)antagonist. TheKivalues 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].

体外研究
(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+]imobilization elicited by 10 nM hU-II with an IC50of 180 nM[2].

Western Blot Analysis[1]

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.
体内研究
(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].

分子量

505.81

性状

Solid

Formula

C19H22BrClN2O5S

CAS 号

474960-44-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month