小分子靶点筛选 > 小分子探针修饰
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小分子探针修饰

小分子探针修饰是化学蛋白质组学和药物靶点发现中的关键技术,通过在活性药物分子结构中引入特定功能基团,实现对药物分子靶点富集鉴定和定位分析。针对天然产物、内源性代谢物、化学药物及多糖等不同类型分子,达吉特均可根据其结构进行评估修饰,为解析药物作用机制、发现未知结合蛋白及开展靶点验证提供可靠工具。

达吉特的化学合成专家团队具有多年的天然产物从头合成经验,可以根据小分子的结构优化合成反应设计,实现特定位点的定点修饰,并确保产物的质量与纯度达到最佳。

|  达吉特小分子探针标记服务独特优势

修饰经验:达吉特已完成上干种小分子的各类修饰,包括生物素、炔基、光交联基团及荧光等。同时,达吉特常备300+种炔基和光交联基团标记的小分子现货产品,可满足不同研究需求。

图1-小分子探针修饰-吴茱萸碱.jpg

质控保证:达吉特提供的小分子探针修饰产品均会进行核磁氢谱和质谱的鉴定检测,在保证结构正确的同时,会将产物纯度提高到95%以上,以符合药物研究各项基本需求。

图2-质谱+核磁氢谱-吴茱萸碱.png

|  客户案例

客户案例1:淫羊藿苷(Icariin) CAS:489-32-7

标记策略:作为多功能的黄酮苷类化合物,淫羊藿苷能增加心脑血管血流量、促进造血功能、免疫功能及骨代谢,具有补肾壮阳、抗衰老、抗肿瘤等功效。在对淫羊藿苷进行标记时,我们利用分子中不同类型羟基存在不同反应活性的特点,特异性将丁二酸修饰于糖苷伯醇上,再利用生物素-PEG-胺基进行标记。该策略的优势在于PEG链的引入大大增加了分子的脂溶性和水溶性,此外生物素部分还与活性分子之间存在较远的距离,对分子活性的影响大大降低,有利于后续标记实验的顺利开展。

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客户案例2:芍药苷(Paeoniflorin)CAS: 23180-57-6 

标记策略:作为一种从芍药根中分离出的活性糖苷化合物,芍药苷已被发现具有治疗阿尔茨海默症、帕金森病和癫痫等疾病的潜力。此外,它还显示出抗肿瘤活性,以及对类风湿关节炎和强直性脊柱炎等自身免疫性疾病的治疗作用。 在对芍药苷进行标记时,我们利用分子中糖苷伯羟基高反应活性的特点,实现生物素-PEG-羧基的特异性标记。该策略的优势在于PEG链的引入大大增加了分子的脂溶性和水溶性,并且生物素部分与芍药苷分子通过PEG连接链相连,距离较远,大大降低了对芍药苷分子活性的影响,有利于后续标记实验的顺利开展。 

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客户案例3:丹参素钠(Sodium danshensu)CAS:67920-52-9

标记策略:丹参素为丹参所含专属性成分,其钠盐具有心肌保护,抑制血栓,抗炎、增强免疫、抗血小板聚集等药理活性。 在对丹参素钠进行标记时,我们利用分子中的羧基进行生物素-PEG-胺基的特异性标记。该策略的优势在于PEG链的引入大大增加了分子的脂溶性和水溶性,并且新生成的酰胺键结构稳定,有利于后续标记实验的顺利开展。

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——   客 户 文 献  ——

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