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- Levosimendan 141505-33-1

- Levosimendan 141505-33-1
Levosimendan 141505-33-1
产品描述 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.纯度 99%储存/保存方法 Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.基本信息 别名 左xi孟旦;OR1259外观 yellow可溶性/溶解性 DMSO : 52 mg/mL (185.5 mM)生物活性 靶点 Cardiac troponin CIn vitro(体外研究) Levosimendan is a calcium sensitizer acting through calcium-dependent binding to cardiac troponin C (cTnC). Levosimendan at 3 μM decreases the value of Ca50 from 2.73μM to 1.19 μM. levosimendan exhibits its calcium sensitizing effect through calcium-dependent binding to the N-terminal domain of cTnC. Levosimendan significantly hyperpolarizes resting potential of rat mesenteric arterial myocytes with an EC50 of 2.9 μM and maximal effect (19.5 mV) at 10 μM, probably through activation of a glibenclamide-sensitive K+ channel. Levosimendan has inotropic and lusitropic actions in failing human myocardium, with average maximum increase in twitch tension of 47% at a levosimendan concentration of 0.8 μM. Levosimendan causes rapid dose-dependent improvement in hemodynamic function in patients with decompensated heart failure.In vivo(体内研究) Levosimendan at low concentrations (0.03 to 0.1 μM) acts preferably as a Ca2+ sensitizer, whereas at higher concentrations (0.1 to 0.3 μmol/L) its action as a phosphodiesterase inhibitor contributes to the positive inotropic effect.参考文献 参考文献 1. Haikala H, J Mol Cell Cardiol, 1995, 27(9), 1859-1866.
2. Yokoshiki H, Eur J Pharmacol, 1997, 333(2-3), 249-259.
研究领域 研究领域 CardiovascularDrug DiscoverySmall Molecule DrugLead Compound DiscoveryLevosimendan 141505-33-1温馨提示:本产品仅作科研实验使用,不支持临床等研究
