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  4. GSK812397

GSK812397是一种CXCR4拮抗剂，对HIV感染的抑制具有潜力。为了评估GSK812397的临床潜力，需要公斤级别的试剂候选物。本文描述了CXCR4拮抗剂GSK812397的改进型、可扩展的合成路线。这一新路线已在50升固定设备中放大，以在五步反应中以20%的总产率和>99%的化学纯度及对映体纯度获得1.2公斤试剂物质。CXC趋化因子受体4（CXCR4）是一种7跨膜蛋白，部分作为HIV-1多种菌株的宿主共受体发挥作用。人们认为，针对CXCR4将有助于抑制几种细胞病变晚期病毒的复制；因此，CXCR4拮抗剂是实验性抗HIV试剂最有前途的新类之一。GSK812397是一种强效的CXCR4拮抗剂，因此是抑制HIV感染的研究对象。

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GSK812397 Chemical Structure

GSK812397 Chemical Structure

CAS No. : 878197-98-9

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GSK812397 相关抗体

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  • 生物活性

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生物活性

GSK812397 is a CXCR4 antagonist with potential for the treatment of HIV infection. To evaluate the clinical potential of GSK812397, kilogram-scale agent candidates are needed. Here, an improved, scalable synthetic route for the CXCR4 antagonist GSK812397 is described. This new route has been scaled up in a 50-liter stationary facility to obtain 1.2 kg of agent substance in 20% overall yield and >99% chemical and enantiomeric purity in five steps. CXC chemokine receptor 4 (CXCR4) is a 7-transmembrane protein that functions in part as a host co-receptor for multiple strains of HIV-1. It is thought that targeting CXCR4 will help inhibit the replication of several late cytopathic viruses; therefore, CXCR4 antagonists are one of the most promising new classes of experimental anti-HIV agents. GSK812397 is a potent CXCR4 antagonist and is therefore a candidate for investigation for the treatment of HIV infection.

分子量

420.55

Formula

C24H32N6O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

GSK812397 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK812397878197-98-9GSK 812397GSK-812397OthersInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-111224
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