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YM-244769 dihydrochloride  

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产品描述：基本信息 产品编号： Y10042 产品名称： YM-244769 dihydrochloride CAS: 1780390-65-9   储存条件 粉末 -20℃ 四年 分子式： C26H24Cl2FN3O3 溶于液体 -80℃ 二年 分子量： 516.39     化学名：  N-[(3-Aminophenyl)methyl]-6-[4-[(3-fluorophenyl)methoxy]phenoxy]-3-pyridinecarboxamide dihydrochloride 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 一种有效的钠钙交换体(Na+/Ca2+exchange;NCX)抑制剂，YM-244769dihydrochloride优先抑制NCX3(IC50=18nM)。YM-244769dihydrochloride具有神经和肾脏保护。 靶点 Na+/Ca2+Exchanger   体外研究 YM-244769 preferentially inhibits intracellular Na+-dependent 45Ca2+uptake via NCX3 (IC50=18nM);the inhibition is 3.8-to 5.3-fold greater than for the uptake via NCX1 or NCX2,but it does not significantly affect extracellular Na+-dependent 45Ca2+efflux via NCX isoforms.YM-244769 (0.003-1μM) inhibits dose dependently the initial rates of 45Ca2+uptake into NCX1,NCX2,and NCX3 transfectants with IC50 values of 68±2.9,96±3.5,and 18±1.0nM,respectively,indicating that YM-244769 is approximately four to five times more selective to NCX3 than other isoforms.YM-244769 (0.3 or 1μM) efficiently suppresses the hypoxia/reoxygenation-induced cell damage in SH-SY5Y cells treated with NCX1 antisense (i.e.,SH-SY5Y cells primarily expressing NCX3) more than in those treated with NCX3 antisense (i.e.,SH-SY5Y cells primarily expressing NCX1). Cell Viability Assay Cell Line: SH-SY5Y cells treated with NCX1 or NCX3 antisense Concentration: 0.3 and 1μM Result: Hypoxia/reoxygenation-induced LDH release was significantly attenuated:reduction in cell damage was greater in cells treated with NCX3 antisense (by 61%) than in cells treated with NCX1 antisense (by 35%).0.3 or 1μM efficiently suppressed the hypoxia/reoxygenation-induced cell damage in SHSY5Y cells treated with NCX1 antisense more than in those treated with NCX3 antisense.
保存条件：-20℃

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