Levosimendan

Synonyms: OR1259,OR1855,Simsndan

Levosimendan(OR1259,OR1855,Simsndan) is a calcium sensitizer acting through calcium-dependent binding to cardiac troponin C (cTnC), provides treatment for heart failure.

Levosimendan Chemical Structure

Levosimendan Chemical Structure

CAS No. 141505-33-1

Purity & Quality Control

Levosimendan Related Products

Biological Activity

Description Levosimendan(OR1259,OR1855,Simsndan) is a calcium sensitizer acting through calcium-dependent binding to cardiac troponin C (cTnC), provides treatment for heart failure.
Targets
Cardiac troponin C [1]
In vitro
In vitro

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. [1] 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. [2] 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. [3] Levosimendan causes rapid dose-dependent improvement in hemodynamic function in patients with decompensated heart failure. [4]

In Vivo
In vivo

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. [5]

Animal Research Animal Models guinea pig heart
Dosages 0.03, 0.1, 0.3 μM
Administration administered into the buffer flow line
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04705337 Not yet recruiting
Heart Failure New York Heart Association Class III|Heart Failure New York Heart Association Class IV|Heart Failure Systolic|Heart Failure With Reduced Ejection Fraction
Medical University of Bialystok|Medical Research Agency Poland|University of Opole|Medical University of Lodz|Poznan University of Medical Sciences|Nicolaus Copernicus University|National Institute of Cardiology Warsaw Poland|John Paul II Hospital Krakow|Azienda Ospedaliera dei Colli
January 1 2021 Phase 4
NCT04252404 Completed
Acute Heart Failure
Arcothova
February 3 2020 --
NCT05076864 Recruiting
Pharmacokinetics|Metabolites|Intensive Care|Renal Failure|Acute Kidney Injury
Karolinska Institutet|Karolinska University Hospital
January 1 2020 --
NCT04323709 Completed
Cardiogenic Shock|Refractory Shock
Hospices Civils de Lyon
January 1 2019 --
NCT03681379 Unknown status
Acute Heart Failure
Nantes University Hospital
October 1 2018 --

Chemical Information & Solubility

Molecular Weight 280.28 Formula

C14H12N6O

CAS No. 141505-33-1 SDF Download Levosimendan SDF
Smiles CC1CC(=O)NN=C1C2=CC=C(C=C2)NN=C(C#N)C#N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 56 mg/mL ( (199.8 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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