Levosimendan

Catalog No.S2446

Levosimendan Chemical Structure

Molecular Weight(MW): 280.28

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

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In DMSO USD 610 In stock
USD 97 In stock
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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]
+ Expand
  • Animal Models: guinea pig heart
  • Formulation: Krebs buffer
  • 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 individually and in order:
30% propylene glycol, 5% Tween 80, 65% D5W
30 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
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03022877 Not yet recruiting Myocardial Infarction|Outcome RWTH Aachen University June 2017 --
NCT01720030 Active, not recruiting Acute Kidney Injury VieCuri Medical Centre|Orion Corporation, Orion Pharma September 2016 Phase 2|Phase 3
NCT02640846 Recruiting Septic Shock|Cardiomyopathy Sahlgrenska University Hospital, Sweden December 2015 Phase 4
NCT02531724 Recruiting Acute Kidney Injury|Renal Insufficiency, Acute Sahlgrenska University Hospital, Sweden September 2015 Phase 4
NCT02232399 Recruiting Congenital Heart Defects Göteborg University|Helsinki University Central Hospital October 2014 Phase 2
NCT02025621 Completed Coronary Artery Bypass Grafting|Mitral Valve Surgery|Low Cardiac Output Syndrome Tenax Therapeutics, Inc. July 2014 Phase 3

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Calcium Channel Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID