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MRS 1523  

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产品描述：基本信息 产品编号： M10902 产品名称： MRS 1523 CAS: 212329-37-8   储存条件 粉末 -20℃ 四年 分子式： C23H29NO3S 溶于液体 -80℃ 二年 分子量： 399.55     化学名：  6-Ethyl-5-(ethylsulfanylcarbonyl)-2-phenyl-4-propylpyridine-3-carboxylic acid propyl ester Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   生物活性 产品描述 一种有效的选择性腺苷 A3 受体拮抗剂，对人和大鼠 A3 受体的 Ki 值分别为 18.9nM 和 113nM。在大鼠中，MRS 1523 对 A3 的选择性分别是 A1 和 A2A 受体的 140 倍和 18 倍。MRS 1523 可以通过 N-type Ca channel 阻滞和抑制大鼠背根神经节神经元的动作电位而发挥抗痛觉过敏作用。 靶点 Ki:18.9nM (Human A3 receptor),113nM (Rat A3 receptor),15.6µM (A1 receptor) and 2.05µM (A2A receptor)   体外研究 MRS 1523 (0.1-1μM) treatment significantly antagonizes cell numbers to 40.7% and 57.4% of the control values,respectively,30 min before the addition of cordycepin (60μM).MRS1523 (1μM) alone has any effect on tumor cell growth.A partial blockade of the adenosine-5'-N-ethylcarboxamide (NECA)-induced migration is observed when human endothelial progenitor cells (hEPC) are co-incubated with MRS 1523 (1nM).Furthermore,in 3-days hEPC,the treatment with MRS 1523 100nM inhibits the NECA-induced migration by 70%.NECA-induced migration is blocked in dose-response fashion by MRS 1523 with calculated Ki of 147nM. Cell Viability Assay Cell Line: B16-BL6 cells Concentration: 0.1µM,1µM Incubation Time: 24 hours,48 hours,72 hours Result: Antagonized the growth suppression induced by cordycepin. 体内研究 The expression and functional effects of A3 adenosine receptor (A3AR) on the excitability of small-to medium-sized,capsaicin-sensitive,dorsal root ganglion (DRG) neurons isolated from 3-to 4-week-old rats are investigated.The endogenous agonist adenosine reduces N-type Ca currents,and its effect is inhibited by 56% in the presence of A3AR antagonist MRS 1523.Current-clamp recordings demonstrated that neuronal firing of rat DRG neurons was also significantly reduced by A3AR activation in a MRS 1523-sensitive but PD173212-insensitive manner.
保存条件：-20℃

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