research use only
Cat.No.S2446
| Related Targets | CFTR CRM1 CD markers AChR Sodium Channel Potassium Channel GABA Receptor TRP Channel ATPase GluR |
|---|---|
| Other Calcium Channel Inhibitors | Bay K 8644 Tetrandrine Nilvadipine Flunarizine 2HCl Cilnidipine YM-58483 (BTP2) Ionomycin Imperatorin Manidipine 2HCl Astragaloside A |
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In vitro |
DMSO
: 56 mg/mL
(199.8 mM)
Water : Insoluble Ethanol : Insoluble |
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In vivo |
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| Molecular Weight | 280.28 | Formula | C14H12N6O |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 141505-33-1 | Download SDF | Storage of Stock Solutions |
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| Synonyms | OR1259,OR1855,Simsndan | Smiles | CC1CC(=O)NN=C1C2=CC=C(C=C2)NN=C(C#N)C#N | ||
| Targets/IC50/Ki |
Cardiac troponin C
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|---|---|
| In vitro |
Levosimendan is a calcium sensitizer acting through calcium-dependent binding to cardiac troponin C (cTnC). This compound at 3 μM decreases the value of Ca50 from 2.73μM to 1.19 μM. It exhibits its calcium sensitizing effect through calcium-dependent binding to the N-terminal domain of cTnC. This chemical 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. It 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. This compound causes rapid dose-dependent improvement in hemodynamic function in patients with decompensated heart failure. |
| 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. |
References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| 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 | -- |
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