The present disclosure provides boron-containing diacylhydrazines having Formula I:
and the pharmaceutically acceptable salts and solvates thereof, wherein A, R4, and R5 are defined as set forth in the specification. The present disclosure also provides the use of boron-containing diacylhydrazines is ecdysone receptor-based inducible gene expression systems. Thus, the present disclosure is useful for applications such as gene therapy, treatment of disease, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable.
本公开提供了具有式 I 的含
硼二酰
肼:
及其药学上可接受的盐和溶液,其中 A、R4 和 R5 的定义如说明书所述。本公开还提供了含
硼二酰
肼在基于
蜕皮激素受体的诱导
基因表达系统中的应用。因此,本公开可用于
基因治疗、疾病治疗、蛋白质和
抗体的大规模生产、基于细胞的筛选测定、功能
基因组学、蛋白质组学、代谢组学以及转
基因生物的性状调控等需要控制
基因表达
水平的应用领域。