產(chǎn)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. |
靶點(diǎn): |
Autophagy Carbonic AnhydrasePDE Potassium Channel;PotassiumChannel;PDE;CarbonicAnhydrase;Autophagy |
體內(nèi)研究: |
Levosimendan可使衰竭的人心肌細(xì)胞收縮和松弛,0.8 μM Levosimendan下的抽搐張力平均最大增加47%。Levosimendan可引起代償性心臟衰竭患者體內(nèi)血液動(dòng)力學(xué)函數(shù)快速劑量依賴性增長(zhǎng)。Levosimendan使大鼠腸系膜動(dòng)脈肌細(xì)胞的靜息電位明顯超極化(EC50:2.9 μM),10 μM的作用最大(19.5 mV),這可能是通過(guò)激活格列本脲敏感性K+通道產(chǎn)生的。Levosimendan(3 μM)可使Ca50從2.73 μM減少至1.19 μM |
參考文獻(xiàn): |
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 |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
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: |
部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的權(quán)威性,僅供客戶參考交流研究之用。 |