
簡(jiǎn)要描述:Levosimendan 141505-33-1Levosimendan is a calcium sensitizer used in the management of acutely decompensated congestive heart failure.
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| 品牌 | absin | CAS | 141505-33-1 |
|---|---|---|---|
| 分子式 | C14H12N6O | 純度 | 99% |
| 分子量 | 280.28 | 貨號(hào) | abs47028070 |
| 規(guī)格 | 25mg | 供貨周期 | 現(xiàn)貨 |
| 主要用途 | used in the management of acutely decomp | 應(yīng)用領(lǐng)域 | 化工,生物產(chǎn)業(yè),農(nóng)林牧漁,制藥/生物制藥,綜合 |
Levosimendan 141505-33-1
| 產(chǎn)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. |
| 純度 | 99% |
| 儲(chǔ)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 | |
| 別名 | 左xi孟旦;OR1259 |
| 外觀 | yellow |
| 可溶性/溶解性 | DMSO : 52 mg/mL (185.5 mM) |
| 生物活性 | |
| 靶點(diǎn) | Cardiac troponin C |
| In vitro(體外研究) | 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(體內(nèi)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. |
| 參考文獻(xiàn) | |
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| 研究領(lǐng)域 | |
| 研究領(lǐng)域 | Cardiovascular Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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