| Name | Levosimendan |
| 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. |
| 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.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (7.14 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | Simsndan | PotassiumChannel | Potassium Channel | Phosphodiesterase (PDE) | phosphodiesterase | OR-1855 | OR-1259 | OR 1855 | OR 1259 | Levosimendan | KcsA | Inhibitor | inhibit | Cardiac troponin C | CarbonicAnhydrase | Carbonic Anhydrase | Autophagy |
| Inhibitors Related | Stavudine | Aceglutamide | Hemin | Tamoxifen | Urea | Sodium Dihydrogen Phosphate | D(+)-Raffinose pentahydrate | Guanidine hydrochloride | Hydroxychloroquine | Paeonol | Naringin | Alginic acid |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Neuroprotective Compound Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max | Ion Channel Targeted Library | Anti-Cancer Drug Library |
United States
