antipain | 37691-11-5

• 物质功能分类: 原料药 - 人工合成抗感染类药 - 抗真菌类药
• 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
• 英文名称: antipain
• 英文别名: 2-[[(2S)-5-(diaminomethylideneamino)-1-[[(2S)-1-[[5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopentan-2-yl]carbamoylamino]-3-phenylpropanoic acid
• CAS: 37691-11-5
• 化学式: C₂₇H₄₄N₁₀O₆
• 分子量: 604.71
• InChiKey: SDNYTAYICBFYFH-MAHYXTOZSA-N

物化性质

• 密度：
  1.38

计算性质

• 辛醇/水分配系数(LogP)：
  -2.7
• 重原子数：
  43
• 可旋转键数：
  19
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  283
• 氢给体数：
  9
• 氢受体数：
  8

安全信息

• WGK Germany：
  3

制备方法与用途

生物活性

Antipain 是一种从 Actinomycetes 分离的蛋白酶抑制剂。它能够抑制 N-甲基-N'-硝基-N-亚硝基胍 (MNNG) 诱导的转化，并增加染色体畸变。此外，Antipain 还限制小鼠子宫中 DNA 的合成和功能。

体内研究

完整且处于周期中的雌性小鼠在连续 16 天接受皮下注射 Antipain（3 mg）后，其子宫重量及总 DNA 含量显著减少，与未处理对照组相比具有统计学意义。另外，在第 0 至 120 小时或第 240 至 360 小时之间每 12 小时注射 Antipain（100 μg/g 体重；腹腔注射），显示对抗二甲基亚硝胺诱导的小鼠肺部肿瘤具有抑制作用。

反应信息

• 作为反应物：
  描述：

  putrescine dihydrochloride 、 antipain 在 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 sodium hydroxide 作用下， 以 水 为溶剂， 反应 4.25h， 生成
  参考文献：
  名称：

  Marschuetz; Puttipipatkhachorn; Bernkop-Shnuerch, Pharmazie, 2001, vol. 56, # 9, p. 724 - 729

  摘要：

  DOI：

文献信息

• Protein degradation inducing tag and usage thereof
  申请人：Tokyo University of Science Foundation

  公开号：US10976306B2

  公开（公告）日：2021-04-13

  Provided are: a protein degradation inducing tag which is a molecule that has affinity with proteases and does not inhibit degradation of a protein by proteases; a protein degradation inducing molecule that is a conjugate of at least one protein degradation inducing tag and at least one protein binding molecule that binds to a protein; and a usage of those.

  提供了：一种蛋白质降解诱导标签，它是一种与蛋白酶具有亲和力的分子，不会抑制蛋白酶对蛋白质的降解；一种蛋白质降解诱导分子，它是至少一种蛋白质降解诱导标签和至少一种与蛋白质结合的蛋白质结合分子的共轭物；以及它们的用法。
• P53 degradation inducing molecule and pharmaceutical composition
  申请人：Tokyo University of Science Foundation

  公开号：US11007269B2

  公开（公告）日：2021-05-18

  A p53 degradation inducing molecule which can induce degradation of p53 proteins or p53 composites, and a pharmaceutical composition containing said p53 degradation inducing molecule are provided. This p53 degradation inducing molecule is a conjugate of a p53 affinity molecule which has affinity for p53 proteins or p53 composites, and a proteolysis induction tag which has affinity for protease and which does not inhibit proteolysis of proteins by protease.

  本发明提供了一种可诱导 p53 蛋白或 p53 复合物降解的 p53 降解诱导分子，以及一种含有所述 p53 降解诱导分子的药物组合物。这种 p53 降解诱导分子是对 p53 蛋白质或 p53 复合物具有亲和力的 p53 亲和分子与对蛋白酶具有亲和力且不抑制蛋白酶对蛋白质的蛋白水解的蛋白水解诱导标签的共轭物。
• Ras protein degradation inducing molecule and pharmaceutical composition
  申请人：Tokyo University of Science Foundation

  公开号：US11052154B2

  公开（公告）日：2021-07-06

  A Ras protein degradation inducing molecule that can induce degradation of Ras proteins, and a pharmaceutical composition that contains this Ras protein degradation inducing molecule are provided. The Ras protein degradation inducing molecule is a conjugate of a Ras protein affinity molecule which has affinity to Ras proteins, and a proteolysis-inducing tag which has affinity to protease and does not inhibit proteolysis of proteins by the protease.

  本发明提供了一种可诱导 Ras 蛋白降解的 Ras 蛋白降解诱导分子，以及一种含有这种 Ras 蛋白降解诱导分子的药物组合物。Ras 蛋白降解诱导分子是与 Ras 蛋白亲和的 Ras 蛋白亲和分子和与蛋白酶亲和的蛋白水解诱导标签的共轭物，蛋白水解诱导标签不抑制蛋白酶对蛋白质的蛋白水解。
• BABESIA SUBTILISIN
  申请人：Lobo Cheryl

  公开号：US20090074783A1

  公开（公告）日：2009-03-19

  Provided is an isolated and purified protein produced by a naturally occurring Babesia sp. comprising an amino acid sequence at least 90% identical to SEQ ID NO:1 and an isolated and purified nucleic acid encoding the above protein. Additionally provided is an isolated and purified nucleic acid comprising at least 20 nucleotides having a sequence 100% identical to a portion of SEQ ID NO:2 or its complement. Further provided is an antibody preparation comprising an antibody that specifically binds to the above protein. Also provided are methods of diagnosing a Babesia sp. infection in a mammal, methods of determining whether a blood preparation is contaminated with a Babesia sp., methods of determining whether a blood preparation is contaminated with a Babesia sp., and methods of treating a mammal infected with a Babesia sp., the method comprising inhibiting the production or activity of the protein comprising an amino acid sequence at least 90% identical to SEQ ID NO:1 by the Babesia sp. in the mammal. Additionally provided are methods of screening a compound for treating an infection by a Babesia sp.
• Babesia Subtilisin
  申请人：Lobo Cheryl

  公开号：US20100196380A1

  公开（公告）日：2010-08-05

  Provided is an isolated and purified protein produced by a naturally occurring Babesia sp. comprising an amino acid sequence at least 90% identical to SEQ ID NO:1 and an isolated and purified nucleic acid encoding the above protein. Additionally provided is an isolated and purified nucleic acid comprising at least 20 nucleotides having a sequence 100% identical to a portion of SEQ ID NO:2 or its complement. Further provided is an antibody preparation comprising an antibody that specifically binds to the above protein. Also provided are methods of diagnosing a Babesia sp. infection in a mammal, methods of determining whether a blood preparation is contaminated with a Babesia sp., methods of determining whether a blood preparation is contaminated with a Babesia sp., and methods of treating a mammal infected with a Babesia sp., the method comprising inhibiting the production or activity of the protein comprising an amino acid sequence at least 90% identical to SEQ ID NO:1 by the Babesia sp. in the mammal. Additionally provided are methods of screening a compound for treating an infection by a Babesia sp.