Medetomidine HCl

製品コードS3060 バッチS306001

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

C13H16N2.HCl
分子量 236.74 CAS No. 86347-15-1
Solubility (25°C)* 体外 Water 47 mg/mL (198.53 mM)
Ethanol 47 mg/mL (198.53 mM)
DMSO 12 mg/mL (50.68 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 (126.72mM) 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 Medetomidineは、1.08 nMのKiを持つ選択的α2-adrenoceptorアゴニストであり、α1-adrenoceptorに対して1620倍の選択性を示します。
in vitro Medetomidine is a selectiveα2-adrenoceptor agonist, with Ki of 1.08 nM, exhibits 1620-fold selectivity over α1-adrenoceptor, has very weak or no binding to other neurotransmitter receptors.
in vivo In anesthetized rats, medetomidine (1-100 μg/kg, i.v.) induces a dose-dependent, relatively short-lived reduction in blood pressure and heart rate. In the pithed rat, medetomidine shows very potent vasopressor (PD50 1.7 μg/kg) and sympatho-inhibitory (ID50 1.6 μg/kg) effects without affecting basal heart rate. Medetomidine induces dose-dependent sedation, which at high doses (>100μg/kg) includes loss of the righting reflex and hypothermia. Medetomidine induces a decreases in the turnover rate of biogenic amines in the brain, dose-dependently inhibits norepinephrine (NE) turnover, inhibits brain dopamine turnover at high doses, decreases serotonin turnover.

プロトコル(参考用のみ)

キナーゼアッセイ Receptor binding experiments
Rats are killed and the brains are immediately removed from the skulls, dissected free of the cerebella and homogenized in ice-cold Tris-HC1 buffer. The homogenate is then centrifuged for 5 min at 500 × g at 4 °C and the supernatant fraction is further centrifuged two times at 50,000 × g for 20 min (4 °C), with re-homogenization of the pellet with 20 volumes of fresh buffer followed by centrifugation. The washed pellet is suspensed in Tris-HC1 buffer at approximately 1 and 4 mg protein/ml for [3H]prazosin and [3H]clonidine binding assays, respectively. Binding reaction mixtures contains (in a final volume of 0.5 ml): 50 mM Tris-HC1 (pH 7.7 for [3H]prazosin and pH 7.5 for [3H]clonidine binding assay, respectively), [3H]prazosin 0.5 nM or [3H]clonidine 4 nM, membrane suspension (0.1 ml), ligand to be tested (0.01-0.2 ml) or phentolamine (10 μM) for determination of non-specific binding. MgC12 (10 mM) is also added to the mixture in the [3H]clonidine binding studies. The incubations are performed in triplicate at 25°C for 30 min and are stopped by rapid filtration under suction through Whatman GF/B glass fibre filters followed by three rinses with 5 ml ice-cold buffer. The filters are dried and solubilized in Instagel for 18 h. Radioactivity is counted in a Wallacliquid scintillation counter equipped with external standard and a built-in computer for d.p.m. (disintegration per min) calculation, with reference to standard quench curves for tritium.
動物実験 動物モデル Rat
投薬量 1-100 μg/kg
投与方法 i.v.

参考

  • https://pubmed.ncbi.nlm.nih.gov/2900154/
  • https://pubmed.ncbi.nlm.nih.gov/2880852/
  • https://pubmed.ncbi.nlm.nih.gov/2906007/

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：

Highly Sensitive Label-Free Detection of Small Molecules with an Optofluidic Microbubble Resonator [Li Z, et al. Micromachines, 2018, 9(6)] PubMed: 30424207

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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