Levosimendan

製品コードS2446 バッチS244603

印刷

化学情報

Chemical Structure Synonyms OR1259,OR1855,Simsndan Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C14H12N6O
分子量 280.28 CAS No. 141505-33-1
Solubility (25°C)* 体外 DMSO 56 mg/mL (199.8 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.

溶剤液（一定の濃度）を調合する

生物活性

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

プロトコル(参考用のみ)

キナーゼアッセイ Dansylated troponin C
Recombinant human cTnC is labelled with dansylchloride. Briefly, a solution containing 55 μM cTnC, 10 mM NaHCO3 and 100 mM KCl, at pH 8.0 is gently stirred, while 150 μM dansylchloride is added. The mixture is incubated in the dark for 12 h at 4°C with gentle stirrling. The dansylated protein is then dialyzed, collected by lyophilization and redissolved at a final concentration of 1 μM in acetate buffer containing 10 mM EGTA, at pH 7.0. Fluorescence is measured at 22°C with a Hitachi F-4010 fluoresence spectrophotometer using 340 nm excitation and 502 nm emission wavelength, with a measuring time of 15 s and a bandpass of 5 nm. Calcium chloride is added in 1 mmole increments (total calcium) and the concentration of free Ca2+ is calculated. 3 μM levosimendan is added (from stock solution in DMSO) to the reaction before calcium. Control experiments are performed in the presence of 0.7% DMSO and pH is readjusted to 7.00 with KOH after each Ca2+ addition.
動物実験 動物モデル guinea pig heart
投薬量 0.03, 0.1, 0.3 μM
投与方法 administered into the buffer flow line

カスタマーフィードバック

, , Antiviral Res, 2017, 146:76-85

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Screening of an FDA-approved compound library identifies levosimendan as a novel anti-HIV-1 agent that inhibits viral transcription. [Hayashi T, et al. Antiviral Res, 2017, 146:76-85] PubMed: 28842263

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。