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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.

| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 25 mg | $31 | In Stock | |
| 50 mg | $45 | In Stock | |
| 100 mg | $61 | In Stock | |
| 500 mg | $237 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $39 | In Stock |
| Description | 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. |
| In vitro | Levosimendan caused contraction and relaxation of failing human cardiomyocytes, with a mean maximum increase in twitch tension of 47% at 0.8 μM Levosimendan.Levosimendan induced a rapid dose-dependent increase in hemodynamic functions in patients with compensated heart failure.Levosimendan caused a significant hyperpolarization (EPS) of resting potential (EPS) in rat mesenteric artery myocytes. The resting potential of rat mesenteric artery myocytes was markedly hyperpolarized by Levosimendan (EC50: 2.9 μM), with a maximal effect at 10 μM (19.5 mV), which may be produced by activation of glibenclamide-sensitive K+ channels.Levosimendan (3 μM) reduced the Ca50 from 2.73 μM to 1.19 μM. |
| In vivo | Levosimendan caused contraction and relaxation of failing human cardiomyocytes, with a mean maximum increase in twitch tension of 47% at 0.8 μM Levosimendan.Levosimendan induced a rapid dose-dependent increase in hemodynamic functions in patients with compensated heart failure.Levosimendan caused a significant hyperpolarization (EPS) of resting potential (EPS) in rat mesenteric artery myocytes. The resting potential of rat mesenteric artery myocytes was markedly hyperpolarized by Levosimendan (EC50: 2.9 μM), with a maximal effect at 10 μM (19.5 mV), which may be produced by activation of glibenclamide-sensitive K+ channels.Levosimendan (3 μM) reduced the Ca50 from 2.73 μM to 1.19 μM. |
| Synonyms | OR1855, OR1259 |
| Molecular Weight | 280.28 |
| Formula | 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 |
| Relative Density. | 1.33g/cm3 |
| Color | Yellow |
| Appearance | Solid |
| Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 45 mg/mL (160.55 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (7.14 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
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