PPIase-Parvulin抑制剂 | 64005-90-9

• 物质功能分类: 生物化工 - 抑制剂
• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: PPIase-Parvulin抑制剂
• 英文名称: 1,3,6,8-tetrahydro-1,3,6,8-tetraoxo-benzo[lmn][3,8]phenanthroline-2,7-diacetic acid 2,7-diethyl ester
• 英文别名: PiB；PPIase-Parvulin inhibitor；diethyl 1,3,6,8-tetrahydro-1,3,6,8-tetraoxobenzo[lmn][3,8]phenanthroline-2,7-diacetate；(1,3,6,8-tetraoxo-1,3,6,8-tetrahydro-benzo[lmn][3,8]phenanthroline-2,7-diyl)-bis-acetic acid diethyl ester；(1,3,6,8-tetraoxo-1,3,6,8-tetrahydro-benzo[lmn][3,8]phenanthroline-2,7-diyl)-di-acetic acid diethyl ester；(1,3,6,8-Tetraoxo-1,3,6,8-tetrahydro-benzo[lmn][3,8]phenanthrolin-2,7-diyl)-di-essigsaeure-diaethylester；ethyl 2-[13-(2-ethoxy-2-oxoethyl)-5,7,12,14-tetraoxo-6,13-diazatetracyclo[6.6.2.04,16.011,15]hexadeca-1(15),2,4(16),8,10-pentaen-6-yl]acetate
• CAS: 64005-90-9
• 化学式: C₂₂H₁₈N₂O₈
• 分子量: 438.394
• InChiKey: WNKQGFNIIHNGQM-UHFFFAOYSA-N

物化性质

• 溶解度：
  DMSO：可溶1-2mg/mL（加热）

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  32
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  127
• 氢给体数：
  0
• 氢受体数：
  8

制备方法与用途

用途：该物质可用作生产无灰清净分散剂、粘合剂和绝缘胶的原料，并且也是润滑油添加剂。

反应信息

• 作为产物：
  描述：

  1,4,5,8-萘四甲酸酐 、 2-胺基乙酸乙酯 在 乙醇 作用下， 生成 PPIase-Parvulin抑制剂
  参考文献：
  名称：

  关于萘并咪唑啉的制备

  摘要：

  DOI：

  10.1002/hlca.193802101182

文献信息

• Antioxidants Having Aromatic Structures Reacting with Superoxide
  申请人：Tour James

  公开号：US20160175292A1

  公开（公告）日：2016-06-23

  Disclosed is a method of treating diseases which are: reactive oxygen species mediated, ischemic or reperfusion-related, or T-cell mediated, including autoimmune diseases. The method is administering a therapeutically effective amount of a formulation wherein the active ingredient includes non-phenolic aromatic structures that are electron deficient and are capable of converting the superoxide radical to O 2 ; and/or of converting superoxide radical to oxygen and hydrogen peroxide, or pharmaceutically acceptable salts of said structures. Also disclosed is a method of diagnosing and treating such diseases and conditions.

  本方法揭示了一种治疗疾病的方法，这些疾病包括：由活性氧自由基介导的、缺血或再灌注相关的、或T细胞介导的，包括自身免疫疾病。该方法是向患者施用含有非酚类芳香结构的活性成分的制剂，这些结构是电子不足的并且能够将超氧自由基转化为O2；和/或将超氧自由基转化为氧气和过氧化氢，或者这些结构的药用盐。还揭示了一种诊断和治疗这类疾病和病况的方法。
• Kit for producing a retrovirus with enhanced infectivity
  申请人：Saphire, Andrew C.

  公开号：EP2733213A1

  公开（公告）日：2014-05-21

  The present invention provides kits for carrying out methods for producing retroviruses or viral vectors with enhanced infectivity. The methods entail transfecting a retroviral vector into a packaging cell that has suppressed expression or inhibited enzymatic activity of a parvulin prolyl peptidyl isomerase (parvulin PPIase), and culturing the transfected packaging cell to allow production of viral particles. The invention also provides kits for carrying out methods for enhancing efficiency of gene transfer with a recombinant retrovirus. These methods involve constructing a recombinant retroviral vector expressing a target gene, transfecting into a packaging cell that has suppressed expression or inhibited enzymatic activity of a parvulin prolyl peptidyl isomerase (parvulin PPIase), culturing the transfected packaging cell to allow production of recombinant retroviral particles, harvesting recombinant retroviral particles from supernatant of the cultured cell, and transducing the recombinant retroviral particles into a target cell.

  本发明提供了用于实施生产具有增强感染性的逆转录病毒或病毒载体的方法的试剂盒。这些方法需要将逆转录病毒载体转染到抑制了副粘蛋白脯氨酰肽基异构酶（parvulin prolyl peptidyl isomerase，parvulin PPIase）的表达或酶活性的包装细胞中，并培养转染的包装细胞以产生病毒颗粒。本发明还提供了用于实施提高重组逆转录病毒基因转移效率的方法的试剂盒。这些方法包括构建表达目的基因的重组逆转录病毒载体，转染到抑制了副粘蛋白脯氨酰肽基异构酶（parvulin prolyl peptidyl isomerase，parvulin PPIase）的表达或酶活性的包装细胞中，培养转染的包装细胞以产生重组逆转录病毒颗粒，从培养细胞的上清液中收获重组逆转录病毒颗粒，以及将重组逆转录病毒颗粒转导到目的细胞中。
• METHODS FOR ENHANCING INFECTIVITY OF RETROVIRUSES
  申请人：The Scripps Research Institute

  公开号：EP2432885A2

  公开（公告）日：2012-03-28
• PHARMACEUTICAL COMPOSITIONS AND COMBINATIONS COMPRISING INHIBITORS OF THE ANDROGEN RECEPTOR AND USES THEREOF
  申请人：ESSA Pharma, Inc.

  公开号：US20220218632A1

  公开（公告）日：2022-07-14

  The present disclosure generally relates to pharmaceutical compositions and combinations comprising an androgen receptor N-terminal domain inhibitor or an inhibitor and a second therapeutically active agent, such as an CDK4/6 inhibitor, a Pin1 inhibitor (inhibitor of peptidyl-prolyl cis/trans isomerases), or an antiandrogen. In particular, the present disclosure relates to pharmaceutical compositions and combinations useful for treatment of various cancers, for example breast cancer and prostate cancer. Further, the present disclosure relates administering an androgen receptor N-terminal domain inhibitor in combination with radiation therapy for treatment of various cancers.
• US8802439B2
  申请人：——

  公开号：US8802439B2

  公开（公告）日：2014-08-12