(S)-2-(2-氨基乙酰氨基)-N-(萘-2-基)-3-苯基丙酰胺 | 21438-66-4

• 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: (S)-2-(2-氨基乙酰氨基)-N-(萘-2-基)-3-苯基丙酰胺
• 英文名称: Glycyl-L-phenylalanine 2-naphthylamide
• 英文别名: (2S)-2-[(2-aminoacetyl)amino]-N-naphthalen-2-yl-3-phenylpropanamide
• CAS: 21438-66-4
• 化学式: C₂₁H₂₁N₃O₂
• 分子量: 347.4
• InChiKey: YABDXPBHLDPMOA-IBGZPJMESA-N

物化性质

• 沸点：
  692.4±55.0 °C(Predicted)
• 密度：
  1.254±0.06 g/cm3(Predicted)
• 溶解度：
  在200µlDMSO中溶于100mg。

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  26
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  84.2
• 氢给体数：
  3
• 氢受体数：
  3

安全信息

• 危险品标志：
  Xn
• 安全说明：
  S22,S36
• 危险类别码：
  R40
• 海关编码：
  2924299090

文献信息

• [EN] SMALL MOLECULE AGONISTS OF MUCOLIPIN 1 AND USES THEREOF<br/>[FR] PETITES MOLÉCULES AGONISTES DE LA MUCOLIPINE 1 ET LEURS UTILISATIONS
  申请人：UNIV MICHIGAN REGENTS

  公开号：WO2021041866A1

  公开（公告）日：2021-03-04

  This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a phenyl-sulfonic amide (or similar) structure which function as agonists of mucolipin 1 (ML1), and their use as therapeutics for the treatment of Duchenne muscular dystrophy (DMD) and related disorders.

  这项发明属于药物化学领域。特别是，该发明涉及一类新的小分子，具有苯磺酰胺（或类似）结构，作为肌球脂蛋白1（ML1）的激动剂，以及它们作为治疗杜氏肌肉萎缩症（DMD）和相关疾病的疗法的用途。
• Reagent for testing periodontal diseases
  申请人：SUNSTAR KABUSHIKI KAISHA

  公开号：EP0255341A2

  公开（公告）日：1988-02-03

  A reagent for testing periodontal diseases which diagnoses or prognosticates contraction or progress of said diseases by determining aminopeptidase-like enzymatic activity in a specimen, said reagent comprises as a substrate for the enzyme either or both compounds of the formula: X-Z-Arg-Y [1] wherein Arg is arginine residue; X is hydrogen or an amino blocking group; Y is a color developing group attached to the C-terminal of Arg; and Z is an amino acid or peptide residue composed of 1 to 4 amino acids or their blocked derivatives, the C-terminal of which is attached to the N-­terminal of Arg, and Xʹ-Zʹ-Pro-Yʹ [2] wherein Pro is proline residue; Xʹ is hydrogen or an amino blocking group; Yʹ is a color developing group attached to the C-terminal of Pro; and Zʹ is an amino acid or peptide residue composed of 0 to 4 amino acids or their blocked derivatives, the C-terminal of which is attached to the N-­terminal of Pro.

  一种检测牙周疾病的试剂，它通过测定标本中氨基肽酶样酶的活性来诊断或预测所述疾病的收缩或进展，所述试剂包括作为酶底物的式中的一种或两种化合物： X-Z-Arg-Y [1] 其中 Arg 是精氨酸残基；X 是氢或氨基封端基；Y 是连接到 Arg C 端的显色基团；Z 是由 1 至 4 个氨基酸或其封端衍生物组成的氨基酸或肽残基，其 C 端连接到 Arg 的 N 端，以及 Xʹ-Zʹ-Pro-Yʹ[2］ 其中Pro是脯氨酸残基；Xʹ是氢或氨基封端基；Yʹ是连接到Pro的C-末端的显色基团；Zʹ是由0至4个氨基酸或其封端衍生物组成的氨基酸或肽残基，其C-末端连接到Pro的N-末端。
• Methods and compositions for restoring homeostatic capacity of a subject
  申请人：Palo Alto Investors

  公开号：US10835134B2

  公开（公告）日：2020-11-17

  Methods of restoring homeostatic capacity of a subject are provided. Aspects of the invention further include compositions, systems and devices for practicing the methods. The methods and compositions described herein find use in a variety of applications. Aspects of certain embodiments of the methods include modulating a subject's autonomic nervous system in a manner sufficient to restore the homeostatic capacity of the subject. Aspects of other embodiments of the invention include administering to the subject an amount of an apoptosis modulator effective to at least partially restore homeostatic function of the neuroendocrine system of the subject.

  本发明提供了恢复受试者体内平衡能力的方法。本发明的各个方面还包括用于实施这些方法的组合物、系统和设备。本文所述的方法和组合物可用于多种应用。本发明方法的某些实施方案包括以足以恢复受试者平衡能力的方式调节受试者的自律神经系统。本发明其他实施方案的方面包括向受试者施用一定量的细胞凋亡调节剂，其有效量至少可部分恢复受试者神经内分泌系统的平衡功能。
• METHOD AND COMPOSITION FOR THE TREATMENT OF CANCER BY THE ENZYMANTIC CONVERSION OF SOLUBLE RADIOACTIVE TOXIC PRECIPITATES IN THE CANCER
  申请人：——

  公开号：US20020022003A1

  公开（公告）日：2002-02-21

  A method for the treatment of cancer is disclosed which is capable of directing supra-lethal doses of radiation, called Hot-Spots, virtually exclusively to the cancer. The present invention involves a multi-step therapy process and includes a class of novel chemical agents. In accordance with the present invention, it was discovered that soluble precipitable materials can be made to accumulate as non-digestible precipitates in targeted cells as a result of enzyme action within the targeted cells. Accumulation is achieved by administering to the living host a soluble binary reagent made by attaching a targeting agent to a novel chemical agent which is a soluble precipitable material. The binary reagent binds to antigenic receptors on targeted cells which endocytose the binary reagent and transport it into the lysosomes where enzymes detach the soluble precipitable material from the targeting agent, causing it to precipitate, accumulate, and be retained in the cells. Increasing amounts of precipitate can be made to accumulate in cells by continuing the administration of the binary reagent. The accumulated precipitate is relocated to the extra-cellular fluid by selectively killing a fraction of cancer cells. Now relocated in the extra-cellular fluid of the cancer, the precipitate is used as a “platform” from which to generate Hot-Spots. A bispecific reagent with a non-mammalian enzyme moiety is made to bind to the precipitate. A soluble radioactive material is administered which is converted by the enzyme moiety of the bound bispecific reagent into a new form which is retained adjacent to the precipitate for an extended period of time, thereby generating Hot-Spots which non-selectively kill all cells adjacent to the precipitate in the extra-cellular fluid of the cancer.

  本发明公开了一种治疗癌症的方法，该方法能够将超致命剂量的辐射（称为 "热点"）几乎完全导向癌症。本发明涉及一个多步骤治疗过程，包括一类新型化学制剂。根据本发明，人们发现可溶性沉淀物可以在靶细胞内酶的作用下，以非消化沉淀物的形式在靶细胞内积聚。可溶性沉淀物的积累是通过向活体宿主施用一种可溶性二元试剂来实现的，该试剂是通过将一种靶向药剂与一种新型化学药剂（一种可溶性沉淀物）相连而制成的。二元试剂与靶细胞上的抗原受体结合，靶细胞内吞二元试剂并将其转运到溶酶体中，在溶酶体中酶将可溶性沉淀物与靶向剂分离，使其沉淀、积累并保留在细胞中。通过继续施用二元试剂，可使沉淀物在细胞中的积累量不断增加。通过选择性地杀死一部分癌细胞，可将积累的沉淀转移到细胞外液中。现在，沉淀转移到了癌细胞的细胞外液中，可用作生成热点的 "平台"。一种带有非哺乳动物酶分子的双特异性试剂与沉淀结合。施用一种可溶性放射性物质，这种物质会被结合的双特异性试剂的酶分子转化成一种新的形式，并在沉淀物附近保留较长时间，从而产生热斑，非选择性地杀死癌症细胞外液中沉淀物附近的所有细胞。
• Method and composition for the treatment of cancer by the enzymatic conversion of soluble radioactive toxic agents into radioactive toxic precipitates in the cancer
  申请人：——

  公开号：US20030068382A1

  公开（公告）日：2003-04-10

  A method for the treatment of cancer is disclosed which is capable of directing supra-lethal doses of radiation, called Hot-Spots, virtually exclusively to the cancer. The present invention involves a multi-step therapy process and includes a class of novel chemical agents. In accordance with the present invention, it was discovered that soluble precipitable materials can be made to accumulate as non-digestible precipitates in targeted cells as a result of enzyme action within the targeted cells. Accumulation is achieved by administering to the living host a soluble binary reagent made by attaching a targeting agent to a novel chemical agent which is a soluble precipitable material. The binary reagent binds to antigenic receptors on targeted cells which endocytose the binary reagent and transport it into the lysosomes where enzymes detach the soluble precipitable material from the targeting agent, causing it to precipitate, accumulate, and be retained in the cells. Increasing amounts of precipitate can be made to accumulate in cells by continuing the administration of the binary reagent. The accumulated precipitate is relocated to the extra-cellular fluid by selectively killing a fraction of cancer cells. Now relocated in the extra-cellular fluid of the cancer, the precipitate is used as a “platform” from which to generate Hot-Spots. A bispecific reagent with a non-mammalian enzyme moiety is made to bind to the precipitate. A soluble radioactive material is administered which is converted by the enzyme moiety of the bound bispecific reagent into a new form which is retained adjacent to the precipitate for an extended period of time, thereby generating Hot-Spots which non-selectively kill all cells adjacent to the precipitate in the extra-cellular fluid of the cancer.

  本发明公开了一种治疗癌症的方法，该方法能够将超致命剂量的辐射（称为 "热点"）几乎完全导向癌症。本发明涉及一个多步骤治疗过程，包括一类新型化学制剂。根据本发明，人们发现可溶性沉淀物可以在靶细胞内酶的作用下，以非消化沉淀物的形式在靶细胞内积聚。可溶性沉淀物的积累是通过向活体宿主施用一种可溶性二元试剂来实现的，该试剂是通过将一种靶向药剂与一种新型化学药剂（一种可溶性沉淀物）相连而制成的。二元试剂与靶细胞上的抗原受体结合，靶细胞内吞二元试剂并将其转运到溶酶体中，在溶酶体中酶将可溶性沉淀物与靶向剂分离，使其沉淀、积累并保留在细胞中。通过继续施用二元试剂，可使沉淀物在细胞中的积累量不断增加。通过选择性地杀死一部分癌细胞，可将积累的沉淀转移到细胞外液中。现在，沉淀转移到了癌细胞的细胞外液中，可用作生成热点的 "平台"。一种带有非哺乳动物酶分子的双特异性试剂与沉淀结合。施用一种可溶性放射性物质，这种物质会被结合的双特异性试剂的酶分子转化成一种新的形式，并在沉淀物附近保留较长时间，从而产生热斑，非选择性地杀死癌症细胞外液中沉淀物附近的所有细胞。