Sertraline HCl

製品コードS4053 バッチS405304

印刷

化学情報

Chemical Structure Synonyms CP-51974-1 HCl Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C17H17Cl2N.HCl
分子量 342.69 CAS No. 79559-97-0
Solubility (25°C)* 体外 DMSO 69 mg/mL (201.34 mM)
Ethanol 17 mg/mL (49.6 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
30%PEG400 0.5%Tween80 5%propylene glycol
5.0mg/ml Taking the 1 mL working solution as an example, add 300 μL of 16.67 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O Dilute to 1 mL. 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 Sertraline HCl (CP-51974-1) is a 5-HT antagonist with Ki of 13 nM.
in vitro Sertraline exhibits better selectivity for inhibiting 5-HT uptake relative to NE uptake than fluvoxamine, zimelidine, norzimelidine, fluoxetine or chlorimipramine. However, Sertraline is less selective for blocking 5-HT uptake, relative to DA uptake than these agents. [1]
in vivo Sertraline HCl (32μmol/kg i.p.) inhibits serotonin uptake into striatal synaptosomes from rats by more than 50%. Sertraline HCl is 6 times more potent than chlorimipramine and 60 times more potent than amitriptyline in reversing the 5-HT depletion elicited by PCA. Acute and repeated dosing of sertraline decreased serotonin content of whole blood. Sertraline HCl strongly reduces immobility of mice in the Porsolt swim test for antidepressants. After repeated dosing in rats, sertraline HCl diminishes the cyclic AMP response of limbic forebrain adenylate cyclase to norepinephnne, as well as the binding of [3H]dihydroalprenolol to cortical membranes. [1]

プロトコル(参考用のみ)

キナーゼアッセイ Affinity determination
Rats are decapitated, and brains are immediately dissected to remove corpus stniatum or hypothalamus according to Glowinski and Iversen (1966). Tissue is homogenized (25 ml/g) in ice-cold 0.32 M sucrose solution which also contained glucose (1 mg/ml), 0.0001 M disodium (ethylenediamine)tetraacetate (EDTA) and sufficient Fisher tnis (hydroxymethyl)aminomethane to achieve pH 7.4. A motor-driven Teflon pestle (0.5-mm clearance) and glass homogenizer are used. The homogenate is centnifuged at 1000 g for 10 minutes at 0-4℃, and the supernatant is recentnifuged at 17,000 g for 20 minutes. The pellet is gently resuspended in the ice-cold sucrose solution. For incubations, the following buffer is prepared: 26 mM Tnis hydrochloride buffer, pH 7.4, containing: NaCI (124), KC1 (4.5), KH2P04 (1.2), MgCl2•6H2O (1.3), ascorbic acid (0.001), nialamide hydrochloride (0.0125) and CaCl2 (2.8) added just after adjusting pH with hydrochloric acid. The incubation mixture is comprised of 1 ml of this buffer containing the 14C-labeled monoamine (0.1μM) and glucose (1 mg/ml), 10 on 20 ı of inhibitor solution and 0. 1 ml of the synaptosomal preparation. Ten-minute incubations are carried out sequentially at 37℃, followed by filtration through Millipone filters. After washing with 10 ml of the pH 7.4 buffer, the filters are dried on a hot plate glass counting vials, treated with 7.5-mi of Aquasol until translucent and counted for radioactivity in a Nuclear-Chicago Mark I scintillation counter is determined by the method of Lowry et al (1951). Six concentrations in duplicate of each inhibitor are routinely run, and the concentration blocking uptake by 50% (1C50) is estimated on log probit paper (Horn et al., 1971).
動物実験 動物モデル Rats, Mice
投薬量 --
投与方法 i.p.

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：

Inhibition of Arenaviruses by Combinations of Orally Available Approved Drugs [ Antimicrob Agents Chemother, 2021, AAC.01146-20] PubMed: 33468464
Effect of SSRI exposure on the proliferation rate and glucose uptake in breast and ovary cancer cell lines [ Sci Rep, 2021, 11(1):1250] PubMed: 33441923
In vitro activity of non-antibiotic drugs against Staphylococcus aureus clinical strains [ J Glob Antimicrob Resist, 2021, 27:167-171] PubMed: 34560306

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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