Acebutolol HCl

製品コードS4010 バッチS401002

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C18H28N2O4.HCl

 
分子量 372.89 CAS No. 34381-68-5
Solubility (25°C)* 体外 DMSO 74 mg/mL (198.44 mM)
Water 74 mg/mL (198.44 mM)
Ethanol 74 mg/mL (198.44 mM)
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.
Clear solution
Saline

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。

 30.000mg/ml (80.45mM) Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, 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 Acebutolol is a β-adrenergic receptors antagonist used in the treatment of hypertension, angina pectoris and cardiac arrhythmias.
in vitro Acebutolol inhibits NA uptake in rat brain P2 fractions with IC50 of 0.25 mM. [1] Acebutolol produces a concentration-dependent inhibition of 125I-labeled CYP binding to human fat cell membranes and are able to completely displace all specifically bound radioligand. Acebutolol totally inhibits lipolytic activity initiated by 1 μM isoproterenol. Acebutolol is a cardioselective antagonist possessing low lipid solubility. [2] Acebutolol, which does not bind to LDL, shows a stronger inhibiting effect on the intracellular accumulation of cholesterol esters in J774 macrophages than alprenolol and oxprenolol which bind to LDL. [3]
in vivo Acebutolol following single intravenous administration (10 mg/kg) to rat results in the plasma clearance of 61.9 mL/min/kg, the volume of distribution of 9.6 L/kg, and an elimination half-life of 1.8 hours. Acebutolol following single intravenous administration (50 mg/kg) to rat results in the plasma clearance of 46.5 mL/min/kg, the volume of distribution of 9.5 L/kg, and an elimination half-life of 2.3 hours. [4] Acebutolol (30 mg/kg) decreases cardiac output by 65% and 31% after 1 min and 10 min measurements, respectively, in Sprague-Dawley rats. Acebutolol (30 mg/kg) significantly reduces regional blood flow (RBF) in most organs either after 1 min or 10 min measurements when compare with the baseline values in Sprague-Dawley rats. [5]
特徴 Acebutolol has stabilizing and quinidine-like effects on cardiac rhythm as well as weak inherent sympathomimetic action.

プロトコル(参考用のみ)

動物実験 動物モデル Sprague–Dawley rats
投薬量 10 mg/kg
投与方法 Intravenously

参考

  • https://pubmed.ncbi.nlm.nih.gov/6148250/
  • https://pubmed.ncbi.nlm.nih.gov/2900871/
  • https://pubmed.ncbi.nlm.nih.gov/9032944/
  • https://pubmed.ncbi.nlm.nih.gov/9267686/
  • https://pubmed.ncbi.nlm.nih.gov/11180190/

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：

Evaluation of CML TKI Induced Cardiovascular Toxicity and Development of Potential Rescue Strategies in a Zebrafish Model [ Front Pharmacol, 2021, 12:740529] PubMed: 34733159

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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