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SB-657510

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Chemical Structure| 474960-44-6 同义名 : -
CAS号 : 474960-44-6
货号 : A1209761
分子式 : C19H22BrClN2O5S
纯度 : 97%
分子量 : 505.81
MDL号 : MFCD16618389
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(207.59 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 SB-657510 is a selective urotensin II receptor antagonist. The Ki values for human, monkey, cat, rat and mouse receptors are 61, 17, 30, 65 and 56 nM, respectively. SB-657510 inhibits UII-induced up-regulation of inflammatory mediators (e.g., adhesion molecules, cytokines, and tissue factors in human vascular endothelial cells), thereby exerting anti-inflammatory effects]1][2].SB-657510 significantly blocked the UII-induced increase in adhesion between U937 cells and EA.hy926 cells. At a concentration of 1 μM for 0.5-8 hours, SB-657510 blocked UII-induced tissue factor expression in endothelial cells[1].SB-657510 inhibited [Ca2+]i migration induced by 10 nM hU-II in the concentration range of 1-10000 nM with an IC50 value of 180 nM[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.98mL

0.40mL

0.20mL

9.89mL

1.98mL

0.99mL

19.77mL

3.95mL

1.98mL
参考文献

[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 Jul 30;21(4):277-83.

[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 Oct;155(3):374-86.

[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 May;56(5):1155-65.