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Levosimendan

Name: Levosimendan
Brand: TargetMol
SKU: T2530
Price: 31 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T2530Cas No. 141505-33-1

Alias OR1855, OR1259

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.

Levosimendan

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Purity: 99.91%

Catalog No. T2530Alias OR1855, OR1259Cas No. 141505-33-1

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$31	In Stock	In Stock
50 mg	$45	In Stock	In Stock
100 mg	$61	In Stock	In Stock
500 mg	$237	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$39	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.91%

Color:Yellow

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Product Introduction

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

Bioactivity

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

Chemical Properties

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

Storage & Solubility Information

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: 250 mg/mL (891.97 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.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.5679 mL	17.8393 mL	35.6786 mL	178.3930 mL
5 mM	0.7136 mL	3.5679 mL	7.1357 mL	35.6786 mL
10 mM	0.3568 mL	1.7839 mL	3.5679 mL	17.8393 mL
20 mM	0.1784 mL	0.8920 mL	1.7839 mL	8.9197 mL
50 mM	0.0714 mL	0.3568 mL	0.7136 mL	3.5679 mL
100 mM	0.0357 mL	0.1784 mL	0.3568 mL	1.7839 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc