产品描述: | Levosimendan is a calcium sensitizer used in the management of acutely decompensated congestive heart failure. It increases the sensitivity of the heart to calcium, thus increasing cardiac contractility without a rise in intracellular calcium. Levosimendan exerts its effect by increasing calcium sensitivity of myocytes by binding to cardiac troponin C in a calcium-dependent manner. |
靶点: |
Autophagy Carbonic AnhydrasePDE Potassium Channel;PotassiumChannel;PDE;CarbonicAnhydrase;Autophagy |
体内研究: |
Levosimendan可使衰竭的人心肌细胞收缩和松弛,0.8 μM Levosimendan下的抽搐张力平均最大增加47%。Levosimendan可引起代偿性心脏衰竭患者体内血液动力学函数快速剂量依赖性增长。Levosimendan使大鼠肠系膜动脉肌细胞的静息电位明显超极化(EC50:2.9 μM),10 μM的作用最大(19.5 mV),这可能是通过激活格列本脲敏感性K+通道产生的。Levosimendan(3 μM)可使Ca50从2.73 μM减少至1.19 μM |
参考文献: |
1.Hasenfuss G, Circulation, 1998, 98(20), 2141-2147. 2.Yokoshiki H, Eur J Pharmacol, 1997, 333(2-3), 249-259. 3.Edes I, Circ Res, 1995, 77(1), 107-113. 4.Haikala H, J Mol Cell Cardiol, 1995, 27(9), 1859-1866. 5.Slawsky MT, Circulation, 2000, 102(18), 2222-2227. |
溶解性: |
Ethanol:<1 mg/mL DMSO:52 mg/mL (185.5 mM) H2O:<1 mg/mL |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
3.568 ml |
17.839 ml |
35.678 ml |
5 mM |
0.714 ml |
3.568 ml |
7.136 ml |
10 mM |
0.357 ml |
1.784 ml |
3.568 ml |
50 mM |
0.071 ml |
0.357 ml |
0.714 ml |
|
注意: |
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