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Levosimendan
Synonyms: 左西孟旦, OR1855, OR1259货号 T2530Cas号 141505-33-1 一键复制产品信息纯度: 99.91%
很棒
很棒Levosimendan (OR1259) 是一种钙增敏剂，通过以钙依赖性方式与心肌肌钙蛋白 C 结合，增加肌细胞对钙的敏感性来发挥其作用，可治疗急性失代偿性充血性心力衰竭。
Levosimendan
一键复制产品信息 很棒纯度: 99.91%
货号 T2530Cas号 141505-33-1
别名 左西孟旦, OR1855, OR1259
Levosimendan (OR1259) 是一种钙增敏剂，通过以钙依赖性方式与心肌肌钙蛋白 C 结合，增加肌细胞对钙的敏感性来发挥其作用，可治疗急性失代偿性充血性心力衰竭。
其他形式的 “Levosimendan”:
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 5 mg | ¥ 142 | 现货 | |
| 10 mg | ¥ 188 | 现货 | |
| 25 mg | ¥ 285 | 现货 | |
| 50 mg | ¥ 393 | 现货 | |
| 100 mg | ¥ 579 | 现货 | |
| 500 mg | ¥ 2,410 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 288 | 现货 |
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产品介绍
Levosimendan AI Summary
Levosimendan exhibits multiple pharmacological activities. It shows calcium sensitizing activity with an EC50 value exceeding 100,000.0 nM and an inhibitory effect on phosphodiesterase 3 with an IC50 of 8.0 nM. In terms of pharmacokinetics, it has a high level of plasma protein binding (Fu = 0.02), a small volume of distribution at steady state (Vdss = 0.24 L/kg), a short mean residence time (1.1 hr), a short half-life (1.1 hr), and a moderate clearance rate (3.8 mL/min/kg). These properties suggest rapid clearance and limited distribution in the body.
The compound demonstrates anticongestive activity by affecting blood pressure in rats at a dose of 50 mg/kg and displays inhibitory activity against human tyrosyl-DNA phosphodiesterase 1 (TDP1) and the entry of Ebola virus in various screening assays. Additionally, it shows modest antiviral activity against SARS-CoV-2, including inhibition of viral-induced cytotoxicity in Caco-2 and VERO-6 cells. However, the inhibition rates vary and are generally low, such as 2.45% cytotoxicity inhibition in Caco-2 cells at 10 uM and 2.206% inhibition of SARS-CoV-2 3CL-Pro protease at 20 µM.
In assays targeting human HDAC6, Levosimendan exhibits varied inhibition levels, achieving -74.4% inhibition with commercial peptide substrates. It also aids in the prevention of doxorubicin-induced mortality in Zebrafish, showing a dose-dependent increase in survival rate, with the highest activity observed at 40 uM (74.0%).
Overall, Levosimendan shows promise in several therapeutic areas including heart failure, viral infections, and cancer treatment..
Note: Summary generated by AI. Data source: ChEMBL 
生物活性
化学信息
储存&溶解度
| 产品描述 | Levosimendan (OR1259) 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. |
| 体外活性 | Levosimendan（0.03-0.1 μM）是较好的Ca2+增敏剂,而浓度为0.1到0.3 μM时,作为磷酸二酯酶抑制剂,对正性肌力作用有利. |
| 体内活性 | 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。 |
| 别名 | 左西孟旦, OR1855, OR1259 |
| 分子量 | 280.28 |
| 分子式 | C14H12N6O |
| CAS No. | 141505-33-1 |
| Smiles | C[C@H]1C(C2=CC=C(NN=C(C#N)C#N)C=C2)=NNC(=O)C1 |
| 密度 | 1.33g/cm3 |
| 存储 | Shipping with blue ice/Shipping at ambient temperature. 实际储存温度请以COA为准 | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 250 mg/mL (891.97 mM), Sonication is recommended.  H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (7.14 mM), Sonication is recommended. 请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。 | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。 | ||||||||||||||||||||||||||||||||||||
计算器
体内实验配液计算器
请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：
比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL， 一共给药动物10只，您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH2O， 那么您的工作液浓度为2 mg/mL。
母液配置方法：2 mg 药物溶于 100 μL DMSO （ 母液浓度为 20 mg/mL ）, 如您需要配置的浓度超过该产品的溶解度，请先与我们联系。
体内配方的制备方法： 取 100 μL DMSO 母液， 添加 400 μL PEG300 混匀澄清， 再加 50 μL Tween 80, 混匀澄清, 再加 450 μL Saline / PBS / ddH2O 混匀澄清
以上为“体内实验配液计算器”的使用方法举例，并不是具体某个化合物的推荐配制方式，请根据您的实验动物和给药方式选择适当的溶解方案。
剂量转换
对于不同动物的给药剂量换算，您也可以参考 更多
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