RG-102317

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并二恶烷
• 英文名称: RG-102317
• 英文别名: N'-(3,5-dimethylbenzoyl)-N-(2-methyl-3,4-(ethylenedioxy)-benzoyl)-N'-(tert-butyl)hydrazine；N-(5-methyl-1,4-benzodioxan-6-carbonyl)-N'-(tert-butyl)-N'-(3,5-dimethylbenzoyl)hydrazine；N-(3,4-(1,2-ethylenedioxy)-2-methylbenzoyl)-N'-(3,5-dimethylbenzoyl)-N'-tert-butylhydrazine；N-(5-methyl-1,4-benzodioxan-6-carbonyl)-N'-t-butyl-N'-(3,5-dimethylbenzoyl)hydrazine；N-(Tert-butyl)-3,5-dimethyl-N'-[(5-methyl-2,3-dihydro-1,4-benzodioxin-6-YL)carbonyl]benzohydrazide；N'-tert-butyl-N'-(3,5-dimethylbenzoyl)-5-methyl-2,3-dihydro-1,4-benzodioxine-6-carbohydrazide
• 化学式: C₂₃H₂₈N₂O₄
• 分子量: 396.486
• InChiKey: JGJACZABNQGPMT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  29
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.39
• 拓扑面积：
  67.9
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  RG-102317 、 溴化氰 生成 N-cyano-N-(5-methyl-1,4-benzodioxan-6-carbo)-N'-t-butyl-N'-(3,5 -dimethylbenzoyl)hydrazine 、 N-cyano-N-(5-methyl-1,4-benzodioxan-6-carbonyl)-N'-t-butyl-N'-(3,5-dimethylbenzoyl) hydrazine
  参考文献：
  名称：

  摘要：

  DOI：

文献信息

• Bioavailable diacylhydrazine ligands for modulating the expression of exogenous genes via an ecdysone receptor complex
  申请人：Hormann Eugene Robert

  公开号：US20060020146A1

  公开（公告）日：2006-01-26

  The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.

  本发明涉及用于核受体基于诱导基因表达系统的非甾体配体，以及一种调节外源基因表达的方法，其中包括一个包含：DNA结合结构域；配体结合结构域；转活化结构域；和配体的ecdysone受体复合物与包含外源基因和响应元件的DNA构建物接触；其中外源基因受响应元件控制，并且在配体存在的情况下DNA结合结构域与响应元件结合导致基因的激活或抑制。
• BIOAVAILABLE DIACYLHYDRAZINE LIGANDS FOR MODULATING THE EXPRESSION OF EXOGENOUS GENES VIA AN ECDYSONE RECEPTOR COMPLEX
  申请人：Hormann Eugene Robert

  公开号：US20080064741A1

  公开（公告）日：2008-03-13

  The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.

  本发明涉及用于核受体基础诱导基因表达系统的非类固醇配体，以及一种调节外源基因表达的方法，其中包括将一个包含：DNA结合域、配体结合域、转录激活域和配体的ecdysone受体复合物与一个包含：外源基因和响应元件的DNA构建物接触；其中，外源基因在响应元件的控制下，并且在配合剂存在下，DNA结合域与响应元件结合导致基因的激活或抑制。
• Bioavailable Diacylhydrazine Ligands for Modulating the Expression of Exogenous Genes via an Ecdysone Receptor Complex
  申请人：HORMANN Robert Eugene

  公开号：US20120046322A1

  公开（公告）日：2012-02-23

  The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.

  本发明涉及非类固醇配体，用于核受体为基础的可诱导基因表达系统，以及一种调节外源基因表达的方法，其中包括：将一个包含DNA结构的外源基因和响应元件与一个包含：DNA结合域、配体结合域、转录活化域和配体的蜕皮激素受体复合物接触；其中，外源基因受响应元件控制，并在存在配体的情况下，DNA结合域与响应元件结合导致基因的激活或抑制。
• Bioavailable Diacylhydrazine Ligands for Modulations the Expression of Exogenous Genes via an Ecdysone Receptor Complex
  申请人：HORMANN Robert Eugene

  公开号：US20130035487A1

  公开（公告）日：2013-02-07

  The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.

  本发明涉及用于核受体基础诱导基因表达系统的非类固醇配体，以及一种调节外源基因表达的方法，该方法包括：将包括DNA结构的外源基因和响应元件与具有DNA结合域、配体结合域、转录激活域和配体的ecdysone受体复合物接触；其中，外源基因在响应元件的控制下，并且在存在配体的情况下，DNA结合域与响应元件的结合导致基因的激活或抑制。
• Boron-Containing Diacylhydrazines
  申请人：Intrexon Corporation

  公开号：US20150322092A1

  公开（公告）日：2015-11-12

  The present disclosure provides boron-containing diacylhydrazines having Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein R 1 , R 2 , R 3 , R 4 , and R 5 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.

  本公开提供具有I式的含硼二酰肼化合物及其药学上可接受的盐和溶剂化物，其中R1、R2、R3、R4和R5的定义如规范中所述。本公开还提供了使用含硼二酰肼化合物的ecdysone受体基础的诱导基因表达系统。因此，本公开适用于基因治疗、疾病治疗、大规模生产蛋白质和抗体、基于细胞的筛选测定、功能基因组学、蛋白质组学、代谢组学和调控转基因生物的特征等应用，其中需要控制基因表达水平。