Nadolol

製品コードS5023 バッチS502302

印刷

化学情報

 Chemical Structure Synonyms Corgard, Solgol, Anabet, SQ11725 Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C17H27NO4

分子量 309.40 CAS No. 42200-33-9
Solubility (25°C)* 体外 DMSO 62 mg/mL (200.38 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
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

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。

3.1mg/ml (10.02mM) Taking the 1 mL working solution as an example, add 50 μL of 62 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 clarify; 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.
Clear solution
5% DMSO 95% Corn oil

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。

0.45mg/ml (1.45mM) Taking the 1 mL working solution as an example, add 50 μL of 9 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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 Nadolol (Corgard, Solgol, Anabet, SQ11725) is a non-selective beta-adrenergic antagonist with antihypertensive and antiarrhythmic activities.
in vitro Nadolol is a new beta-adrenoceptor blocking agent without intrinsic sympathomimetic action and with an extremely long plasma half life[2]. This compound antagonizes isoproterenol-induced tachycardia and ouabain-induced arrhythmias in cats, antagonizes coronary artery ligation-induced ventricular fibrillation and suppresses ventricular ectopic activity during vagal stimulation in dogs[1].
in vivo In several experimental models (mongrel cats and mongrel dogs), nadolol is effective against cardiac arrhythmias. This anti-arrhythmic activity appears to be related to fi-adrenergic receptor blockade, an action that would antagonize the ability of catecholamines to induce arrhythmias by alteration of cardiac automaticity and conductivity. It is also effective in preventing ventricular fibrillation induced by ligation of the left anterior descending coronary artery. This compound has been demonstrated to have a half-life of 4 to 5 hr in animals. It does not block neuromuscular transmission at the junction of the vagus and heart. Furthermore, this chemical does not depress excitability of the heart, as demonstrated by the lack of effect on diastolic threshold in the intact heart of the dog[1]. It is rapidly absorbed from the gastrointestinal tract and remarkalely well-tolerated when given in extremely large doses[3].

プロトコル(参考用のみ)

動物実験 動物モデル Male mongrel cats, 3.0 to 5.0 kg
投薬量 0.001-0.1 mg/kg
投与方法 i.v.

参考

  • https://www.sciencedirect.com/science/article/pii/001429997690296X
  • https://pubmed.ncbi.nlm.nih.gov/26519/
  • https://pubmed.ncbi.nlm.nih.gov/241655/

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:

Immobilised artificial membrane liquid chromatography vs liposome electrokinetic capillary chromatography: Suitability in drug/bio membrane partitioning studies and effectiveness in the assessment of the passage of drugs through the respiratory mucosa [ J Chromatogr A, 2024, 1734:465286] PubMed: 39191185
Evaluation of an Ussing Chamber System Equipped with Rat Intestinal Tissues to Predict Intestinal Absorption and Metabolism in Humans [ Eur J Drug Metab Pharmacokinet, 2022, 10.1007/s13318-022-00780-x] PubMed: 35733077

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。