Size | Price | Stock | Qty |
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250mg |
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500mg |
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1g |
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2g |
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Other Sizes |
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Levosimendan (trade name Simdax) is a novel and potent calcium sensitizer that has been used in the management of acutely decompensated congestive heart failure.It has a two fold mechanism of action. It leads to greater ionotrophy by increasing the calcium sensitivity as it binds to Troponin and this results in a greater positive iontrophic force. Secondly, the drug is able to open ATP sensitive potassium channels in vascular smooth muscle cells, and the vascular dilatory effects of the drug lead to a decreased pre-load and afterload, putting less work on the heart. This drug is in the process of review by the FDA but has not been approved yet.
ln Vitro |
For the treatment of acute decompensated congestive heart failure, levosimendan (OR1259) is a calcium sensitizer. When traditional treatment is deemed insufficient, levosimendan (OR1259), a dilator, is prescribed for the short-term management of acute decompensated severe chronic heart failure. Levosimendan (OR1259) has demonstrated encouraging first results in a variety of illnesses requiring inotropic support, including as Takotsubo cardiomyopathy, cardiogenic shock, septic shock, and right ventricular failure [1]. Unlike other types of dilators, levosimendan (OR1259) also involves positive energetic and neurohormonal alterations in addition to its distinct drug-receptor interactions for its cardiovascular effects [2]. In adult patients having cardiology and cardiac surgery, levosimendan (OR1259) may lower mortality [3].
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References |
[1]. Nieminen, M.S., et al., Levosimendan: current data, clinical use and future development. Heart Lung Vessel, 2013. 5(4): p. 227-245.
[2]. Papp, Z., et al., Levosimendan: molecular mechanisms and clinical implications: consensus of experts on the mechanisms of action of levosimendan. Int J Cardiol, 2012. 159(2): p. 82-7. [3]. Landoni, G., et al., Effects of levosimendan on mortality and hospitalization. A meta-analysis of randomized controlled studies. Crit Care Med, 2012. 40(2): p. 634-46. |
Molecular Formula |
C14H12N6O
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Molecular Weight |
280.28
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Exact Mass |
280.10726
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CAS # |
141505-33-1
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C1C([H])([H])[C@@]([H])(C([H])([H])[H])C(C2C([H])=C([H])C(=C([H])C=2[H])N([H])/N=C(\C#N)/C#N)=NN1[H]
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Synonyms |
Levosimendanum Simdax Levosimendan
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ≥ 50 mg/mL (~178.39 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.92 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.92 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.5679 mL | 17.8393 mL | 35.6786 mL | |
5 mM | 0.7136 mL | 3.5679 mL | 7.1357 mL | |
10 mM | 0.3568 mL | 1.7839 mL | 3.5679 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.