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）
Clear solution
Saline
30.0mg/ml 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 is a selective α2-adrenoceptor agonist, with Ki of 1.08 nM, exhibts 1620-fold selectivity over α1-adrenoceptor.
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. [1]
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. [2] 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. [3]

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.

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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