首页化合物库天然产物衍生物库
天然产物衍生物库
NATURAL-PRODUCT-BASED LIBRARY

Catalog No.NY1000

天然产物一直是新药研发的宝藏,新结构和新思路的源泉。从20世纪40年代至今,新发现的小分子抗癌药物中有近75%与天然产物相关,1998-2004年间有21种天然产物衍生物在西方国家上市,在随后的5年间,还有19个天然产物衍生物获得批准。很多天然产物及其衍生物都是研究和调节蛋白功能的特效工具。

目前在天然产物研究中有两大机会点:

一是分离纯化出足够多的天然产物单体作为研究样本;

二是一旦研究出感兴趣的单体以后如何进行结构优化,做出成药性更好的系列衍生物。

针对第一点,陶素生物可以提供1880种适合高通量筛选和5100种适合计算机虚拟筛选的天然产物单体库。这些产品都有实体库存,可以快速应用到实验中。

针对第二点,我们对一些热门天然产物骨架尤其是有抗肿瘤,抗病毒潜力的天然产物骨架进行进行了结构优化,得到一系列成药潜力好的化合物,方便客户用更快的时间和更低的成本对相关疾病领域的天然产物研究进行更深入的探求。

天然产物骨架衍生物库以天然产物骨架为基础,通过化学修饰或降解的方法,逐步获得天然产物衍生物。我们以22种极具研究价值的天然产物骨架为基础构建了含有4000个化合物的天然产物衍生物库,是抗肿瘤、抗病毒等研究领域的有力工具,是平台建设多样性的重要部分。

Historically, natural products have been pharma's treasure trove. According to the Natural Products Library Initiative at the Scripps Research Institute, "from 1940s to date, 131 (74.8%) out of 175 small molecule anticancer drugs are natural product-based/inspired, with 85 (48.6%) being either natural products or derived therefrom. From 1981 to date, 79 (80%) out of 99 small molecule anticancer drugs are natural product-based/inspired, with 53 (530/0) being either natural products or derived there from. “In a sense, this is not surprising. In nature, after all, creatures — and at the more basic level, structures, such as receptors and their ligands — have been co—evolving for billions of years.

Pack Size Price
100 μL * 10 mM (in DMSO) RMB 298000.00
100 μL * 10 mM (in DMSO) RMB 298000.00
产品特性
  • 包含22个天然产物骨架,4000个天然产物衍生物;
  • 包含多个子库:基于金雀花碱的子库,基于苦参碱的子库,基于鬼臼毒素的子库,基于特殊生物修饰的天然产物衍生物(如羟脯氨酸,色胺)子库;
  • 所包含的衍生物均是经“Beyond Ro5”筛选的物理化学性质优良的化合物;
  • 无药物—化学限制(剔除掉易反应化合物,毒物等);
  • NMR或LCMS分析保证产品纯度;
  • 所有化合物现货供应,到货快,性价比高。

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包装与存储
  • 形式:可提供1 mg、5 mg的干粉以及DMSO 10 mM浓度的各种规格溶液;
  • 包装:化合物溶液置于带旋盖和二维码的储存管中,后排列于96孔板;
  • 保存:干粉可保存两年;溶于DMSO,-20 °C可保存一年,-80 °C 可保存两年,避免反复冻融;
  • 运输:蓝冰运输。

Despite that sort of a track record, pharma industry was turning away from natural products with the rise of combinatorial chemistry. The most probable reasons for this were:

  • Reluctance in the pharmaceutical industry to investigate natural products because of their structural including stereochemical complexity (strict timelines issue).
  • Challenging isolation of individual compounds from natural sources.
  • Difficulties in analogues synthesis (e.g., for H2L optimization).
  • Negative impact of the key med-chem trends (e.g., Lipinski ROS).
  • Limited accessibility from natural sources and/or difficult synthetic accessibility etc.

Nevertheless. natural products as well as their derivatives continue to play a significant role in the discovery of new approved therapies, as they have done since the earliest days of medicinal research. Thus, Butler highlights that 21 natural-product-derived drugs were approved for use in Western markets during the period 1998-2004 A more recent update to this indicates an additional 19 natural-product-derived approvals during the period January 2005 to April 2010 Natural products have proven successful modulators of difficult targets such as a range of antibacterial targets and, especially, protein—protein interactions Furthermore, many researchers consider natural products and their derivatives as a privileged tools for the study and manipulation of protein function In general, renaissance of the pharma industry interest toward natural products research is observed nowadays since they provide a unique biologically relevant chemical space, especially for difficult, traditionally intractable but nevertheless high value targets.

Many methodologies and approaches have been developed to eliminate the above-mentioned obstacles to research and, accordingly, to a wider application of natural substances in drug discovery. Synthesis of natural-product-derived compounds is one of them. In this case, libraries are generated around a scaffold that is identical to that of the leading natural product and which is obtained by means of chemical modification or degradation- The library members are then synthesized (preferably in combinatorial synthesis mode) from the scaffold using a step-by-step derivatization. The substitution pattern, stereochemistry, and structure of the scaffold may be set as in the natural product itself. This promising approach has been already applied at TargetMol to synthesize small cytosine-based library Furthermore, it has been successfully used to build up more than 4000 members library based on some readily available natural

Product Description
  • The library consists of more than 4,000 members belonging 22 scaffolds (average 180 compounds per scaffold).
  • The library includes the following sub-libraries:
  • Cytisine-based sub-library
  • Matrine-based sub-library
  • Podophyllotoxin-based sub-library
  • Sub-library based on naturally occurring privileged BBS such ashydroxy-prolines, triptamine, nor-tropolone etc.
  • TargetMol "Beyond RO5" filters have been applied for the library population (See Phys-chem parameters for the library members).
  • NO Med-Chem restrictions (widely accepted and proprietary TargetMol substructure filters on reactive functionalities, toxicophoric, instability suspicions etc.).
  • More than 90% purity for each library member confirmed by LC-MS or NMR analysis.
陶素化合物库特点:
  • 详细的化学结构
  • 二维码储存管
  • 蓝冰干冰运输
  • NMR和HPLC保证产品纯度

默认产品规格为:
  • 1mg/well (powder)
  • 100μL/well (10mM solution)
  • 250μL/well (10mM solution)

* 产品高度可定制化,用户可以选择自己的化合物组库。
技术支持
在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-998-7375,或者邮箱 info@tsbiochem.com,直接联系到我们。我们会在24小时内尽快联系您。
订购方式
联系陶素
电话:400-821-2233
传真:021-34692979
邮箱:info@tsbiochem.com


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