Pimobendan

製品コードS1550 バッチS155001

印刷

化学情報

Chemical Structure Synonyms UD-CG 115 BS Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C19H18N4O2
分子量 334.37 CAS No. 74150-27-9
Solubility (25°C)* 体外 DMSO 67 mg/mL (200.37 mM)
Ethanol 5 mg/mL (14.95 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension
0.5% methylcellulose

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 10.000mg/ml (29.91mM) Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 0.5% methylcellulose clear solution, and mix evenly to form a uniform suspension. 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 Pimobendan (UD-CG 115 BS) is a selective inhibitor of PDE3 with IC50 of 0.32 μM.
in vitro Pimobendan exhibits selective inhibition of PDE III isolated from guinea pig cardiac muscle with IC50 of 0.32 uM compared to the inhibition of PDE I and PDE II (IC50s >30 μM). [1] This compound inhibits the activity of cAMP-PDE III with IC50 of 2.4 μM. It also exerts concentration-dependent positive inotropic effects in isolated guinea-pig papillary muscles with a potency (EC50) of 6.0 μM, which is partly due to selective cardiac PDE III inhibition. [2] In human atrial cells, 100 μM of this chemical significantly increases the L-type calcium current (ICa(L)) (evoked by depolarization to +10 mV from a holding potential of -40 mV) by 250.4% with the half-maximal stimulation (EC50) of 1.13 μM. In rabbit atrial cells, it increases ICa(L) at +10 mV by 67.4.%, which is significantly lower than that obtained in human atrial cells [3]
in vivo Pimobendan shows a beneficial effect on survival in the murine model of EMC virus-induced myocarditis. Administration of this compound significantly increases the final survival rate from 33.6% (control) to 53.3% (0.1 mg/kg) or 66.7% (1 mg/kg). This chemical (1 mg/kg) also significantly reduces myocardial cellular infiltration, the level of intracardiac tumor necrosis factor (TNF)-α and interleukin (IL)-1β compared with the control group, which shows no effect on myocardial necrosis, heart weight and body weight. It suppresses expression of the intracardiac iNOS gene, causing reduction of intracardiac NO production. [4]

プロトコル(参考用のみ)

キナーゼアッセイ Phosphodiesterase isoenzyme inhibition
The isoenzymes PDE I, PDE II and PDE III are isolated from left ventricular guinea pig muscle. For determination of enzyme inhibition, Pimobendan is preincubated for 5 minutes with PDE in a buffer containing 40 mM Tris HCl, 50 mM MgCl2, and 10 mM EGTA (PH 8.0). The reaction is initiated at 37 °C by adding 0.3 μM [3H]cAMP (or 2.5 μM [3H]cGMP in the case of PDE II). The concentration of PDE is such that only 10% of the substrate is hydrolyzed during the reaction, which is stopped after 20 minutes by heating to 90 °C briefly. The reaction product [3H]AMP is split to [3H]adenosine by a phosphatase from king cobra venom. [3H]adenosine is separated from unhydrolyzed [3H]cAMP by chromatography and quantified in a scintillation counter. The concentration that produces 50% inhibition of hydrolysis (IC50) is determined from concentration-response curves.
動物実験 動物モデル Male DBA/2 mice of viral myocarditis
投薬量 0.1 or 1 mg/kg
投与方法 Orally once daily

参考

  • https://pubmed.ncbi.nlm.nih.gov/1719287/
  • https://pubmed.ncbi.nlm.nih.gov/2549430/
  • https://pubmed.ncbi.nlm.nih.gov/9283687/
  • https://pubmed.ncbi.nlm.nih.gov/10193745/

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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。

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