Levosimendan

For research use only.

Catalog No.S2446

1 publication

Levosimendan Chemical Structure

CAS No. 141505-33-1

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

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10mM (1mL in DMSO) EUR 599 In stock
EUR 95 In stock
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Selleck's Levosimendan has been cited by 1 publication

1 Customer Review

  • (B-E) The % of GFP-positive cells upon compound treatment were determined for the indicated HIV-1 latency cell lines (B. J-LAT 6.3; C. JLAT 10.6; D. CA5; E. EF7). Results were normalized to DMSO control. Values represent the mean ± s.d. (n = 4-6). * p < 0.05, one-way ANOVA followed by Tukey’s multiplecomparison test

    Antiviral Res, 2017, 146:76-85. Levosimendan purchased from Selleck.

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Biological Activity

Description Levosimendan 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

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 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]

Protocol

Animal Research:[5]
- Collapse
  • Animal Models: guinea pig heart
  • Dosages: 0.03, 0.1, 0.3 μM
  • Administration: administered into the buffer flow line
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 56 mg/mL (199.8 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+40%PEG 300+5%Tween80+50%ddH2O
For best results, use promptly after mixing.
5 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 280.28
Formula

C14H12N6O

CAS No. 141505-33-1
Storage powder
in solvent
Synonyms N/A
Smiles CC1CC(=O)NN=C1C2=CC=C(C=C2)NN=C(C#N)C#N

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04252404 Not yet recruiting -- Acute Heart Failure Arcothova January 28 2020 --
NCT04323709 Completed Other: Data collection|Other: Data analysis Cardiogenic Shock|Refractory Shock Hospices Civils de Lyon January 1 2019 --
NCT03681379 Not yet recruiting -- Acute Heart Failure Nantes University Hospital October 1 2018 --
NCT03764722 Recruiting Drug: Levosimendan Systolic Heart Failure Collegium Medicum w Bydgoszczy August 1 2018 Phase 4
NCT03346824 Unknown status -- Cardiogenic Shock University Hospital Strasbourg France November 15 2017 --
NCT03189901 Enrolling by invitation Drug: Regular management+Levosimendan Early Management|Acute Heart Failure|NSTEMI - Non-ST Segment Elevation MI Qilu Hospital of Shandong University July 1 2017 Phase 4

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Calcium Channel Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID