赖氨酰 4-硝基苯胺 | 19826-45-0

• 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: 赖氨酰 4-硝基苯胺
• 中文别名: 赖氨酰4-硝基苯胺
• 英文名称: Lys-pNA
• 英文别名: Lysine 4-nitroanilide；(2S)-2,6-diamino-N-(4-nitrophenyl)hexanamide
• CAS: 19826-45-0；6184-11-8
• 化学式: C₁₂H₁₈N₄O₃
• 分子量: 266.3
• InChiKey: VUUNELJIFNFWJC-NSHDSACASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  19
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  127
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  赖氨酰 4-硝基苯胺 在 水 作用下， 以 丙酮 为溶剂， 生成 4-硝基苯胺
  参考文献：
  名称：

  Polarographic study of hydrolysis of [8-lysine]vasopressin and its derivatives with blood serum of pregnant women

  摘要：

  对孕妇血清中[8-赖氨酸]加压素及一些加压素类激素的水解进行了极谱研究。研究了水解对pH的依赖性（pH最适值：7.4-7.50，底物浓度（Km 1.2 . 10^-5M），pH稳定性和热稳定性。各个加压素类似物的水解速率按顺序递减：[8-赖氨酸]加压素 > Nα-甘氨酰-脯氨酰[8-赖氨酸]-加压素 > Nα-亮氨酰-[8-赖氨酸]加压素 > Nα-丙氨酰-[8-赖氨酸]加压素 > Nα-苯基丙氨酰-[8-赖氨酸]加压素 > Nα-二甘氨酰-[8-赖氨酸]加压素 > Nα-脯氨酰-[8-赖氨酸]加压素 > Nα-三甘氨酰-[8-赖氨酸]加压素 > Nα-肌氨酰基甘氨酰-[8-赖氨酸]加压素。水解程度随着妊娠时间的延长逐渐增加，因为存在催产素。然而，加压素也在非孕妇血清中的酶的作用下被水解，但程度较小。在类似的分析条件下，催产素在非孕妇血清中不被水解，因此催产素比加压素更适合用于极谱测定血清催产素酶。

  DOI：

  10.1135/cccc19801099
• 作为产物：
  描述：

  (S)-1-[(S)-2-((S)-2-Amino-propionylamino)-propionyl]-pyrrolidine-2-carboxylic acid [(S)-5-amino-1-(4-nitro-phenylcarbamoyl)-pentyl]-amide 在 musk melon protease 作用下， 以 水 为溶剂， 生成 赖氨酰 4-硝基苯胺
  参考文献：
  名称：

  Kaneda, Makoto; Yonezawa, Hiroo; Uchikoba, Tetsuya, Bioscience, Biotechnology and Biochemistry, 1997, vol. 61, # 12, p. 2100 - 2102

  摘要：

  DOI：

文献信息

• A 1010 Rate Enhancement of Phosphodiester Hydrolysis by a Dinuclear Aminopeptidase—Transition-State Analogues as Substrates?
  作者：Hyun Ik Park、Li-June Ming

  DOI：10.1002/(sici)1521-3773(19991004)38:19<2914::aid-anie2914>3.0.co;2-p

  日期：1999.10.4

  Streptomyces dizinc aminopeptidase (sAP) shows a specific activity of 33.7 nmol min(-1) mg(-1) toward the hydrolysis of the transition-state analogue bis-p-nitrophenylphosphate with a rate constant of k(cat)/K(m)=100 M(-1) s(-1) and a first-order rate enhancement of about 10(10), which is much superior to several Zn chemical models and comparable to some phosphodiesterases. This study suggests that

  链霉菌二锌氨基肽酶（sAP）对速率为k（cat）/ K（m）的过渡态类似物双-对硝基苯基磷酸酯的水解显示33.7 nmol min（-1）mg（-1）的比活性。 ）= 100 M（-1）s（-1）和约10（10）的一级速率增强，这比几种Zn化学模型要好得多，并且与某些磷酸二酯酶相当。这项研究表明，sAP可以作为一种新型的双核模型系统，以提供对双核水解的进一步了解。
• Purification and Some Properties of an Aminopeptidase from the Seeds of<i>Cannabis sativa</i>
  作者：Kazunari ARIMA、Tetsuya UCHIKOBA、Masayuki SHIMADA、Hiroo YONEZAWA、Makoto KANEDA

  DOI：10.1271/bbb.64.1055

  日期：2000.1

  (HSA) with a molecular mass of 78 kDa was purified from hemp (Cannabis sativa) seeds. The activity was inhibited by monoiodeacetic acid, p-chloromercuri-phenylsulfonic acid, and Zn2+ ion. The specificity of HSA was similar to that of a leucyl aminopeptidase [EC 3.4.11.1] from mammalian cytosol. However, other enzyme properties were different from these of leucyl aminopeptidase.

  从大麻（大麻）种子中纯化出分子量为78 kDa的氨基肽酶（HSA）。活性被单碘乙酸，对氯汞基苯磺酸和Zn2 +离子抑制。HSA的特异性类似于来自哺乳动物细胞质的亮氨酰肽酶[EC 3.4.11.1]。但是，其他酶的性质不同于亮氨酰氨肽酶。
• [EN] PYRROLYDIN-2-ONE DERIVATIVES AS INHIBITORS OF THROMBIN AND FACTOR XA<br/>[FR] DERIVES DE PYRROLYDIN-2-ONE UTILISES COMME INHIBITEURS DE LA THROMBINE ET DU FACTEUR XA
  申请人：GLAXO GROUP LTD

  公开号：WO2004052851A1

  公开（公告）日：2004-06-24

  The invention relates to compounds of formula (I), wherein : R1 represents hydrogen, C1-4 alkyl, -CH2CO2H, -CH2CO2C1-2alkyl, or -CH2CONR7R8; R2 and R3 independently represent hydrogen, -C1-6alkyl, -C1-3alkylCN, -C1-3alkylCO2H, -C1-4alkylOC1-4alkyl, -C1-4alkylS(O)nC1-4alkyl, -C1-4alkylNR10R11, -C1-3alkylNCO2C1-4alkyl, -C1-3alkylCONR7R8, -C1-3alkylCO2C0-2alkylR9, -C1-3alkylCOC0-2alkylR9, -C1-3alkylCON(R8) C0-2 alkylR9, -C1-3alkylNCO2C0-2alkylR9, -C1-3alkylNCOC0-2alkylR9 or -C0-2alkylR9, with the proviso that one of R2 and R3 is hydrogen and the other is a substituent other than hydrogen; n is an integer between 0 and 2; R4 and R5 together with the nitrogen atom to which they are attached form a morpholino ring; R6 represents a group selected from formula (II) wherein T1 and T2 independently represent CH2, NH, S or O with the proviso that when one of T1 or T2 represents NH, S or O the other represents CH2; M represents CH3, -OH or PO; V represents CH or N; W represents H, CH3, Cl or F; X represents C1, Br, F or -CH3; Y represents CH3 or CF3; Z represents -CH3 or F; R7 and R8 are independently hydrogen, C1-4alkyl or together with the N atom to which they are bonded form a 5- or 6- membered non-aromatic heterocyclic ring, optionally containing an additional heteroatom selected from O, N or S; R10 and R11 independently represent C1-4alkyl or together with the N atom towhich they are bonded form a 5- or 6- membered non-aromatic heterocyclic ring, optionally containing an additionalheteroatom selected from O, N or S; R9 represents phenyl or a 5- or 6- membered aromatic or non-aromatic heterocyclic group, containing at least one heteroatom selected from O, N or S, each of which is optionally substituted by 0-2 groups selected from: C1-3alkyl or halogen; and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical condition for which a thrombin inhibitor is indicated.

  该发明涉及式(I)的化合物，其中：R1代表氢，C1-4烷基，-CH2CO2H，-CH2CO2C1-2烷基，或-CH2CONR7R8；R2和R3独立地代表氢，-C1-6烷基，-C1-3烷基CN，-C1-3烷基CO2H，-C1-4烷基OC1-4烷基，-C1-4烷基S(O)nC1-4烷基，-C1-4烷基NR10R11，-C1-3烷基NCO2C1-4烷基，-C1-3烷基CONR7R8，-C1-3烷基CO2C0-2烷基R9，-C1-3烷基COC0-2烷基R9，-C1-3烷基CON(R8) C0-2烷基R9，-C1-3烷基NCO2C0-2烷基R9，-C1-3烷基NCOC0-2烷基R9或-C0-2烷基R9，但要求R2和R3中的一个为氢，另一个为非氢取代基；n是0到2之间的整数；R4和R5与它们连接的氮原子一起形成吗啡环；R6代表从式(II)中选择的基团，其中T1和T2独立地代表CH2，NH，S或O，但要求当T1或T2代表NH，S或O时，另一个代表CH2；M代表CH3，-OH或PO；V代表CH或N；W代表H，CH3，Cl或F；X代表C1，Br，F或-CH3；Y代表CH3或CF3；Z代表-CH3或F；R7和R8独立地代表氢，C1-4烷基，或者与它们连接的N原子一起形成一个5-或6-成员非芳香杂环，选择性地包含另一个从O，N或S中选择的杂原子；R10和R11独立地代表C1-4烷基，或者与它们连接的N原子一起形成一个5-或6-成员非芳香杂环，选择性地包含另一个从O，N或S中选择的杂原子；R9代表苯基或一个5-或6-成员芳香或非芳香杂环基团，其中至少含有一个从O，N或S中选择的杂原子，每个基团选择性地被0-2个从C1-3烷基或卤素中选择的基团取代；以及其药用可接受的衍生物，其制备方法，含有它们的药物组合物以及在医学中的使用，特别是在改善需要凝血酶抑制剂的临床状况中的使用。
• [EN] DUAL-ENZYME RESPONSIVE PEPTIDES<br/>[FR] PEPTIDES SENSIBLES À DEUX ENZYMES
  申请人：UNIV CALIFORNIA

  公开号：WO2018118902A1

  公开（公告）日：2018-06-28

  An enzyme-responsive peptide and a method off using such enzyme-responsive peptide are disclosed. An enzyme-responsive peptide, the peptide comprising an amino acid having an α-amino group, an α-carboxylic acid group and a ε-amine group, wherein the ε-amine group is covalently bonded with a first group and the α-carboxylic acid is covalently bonded with a second group.

  本发明公开了一种酶响应肽和使用该酶响应肽的方法。酶响应肽包括一个具有α-氨基、α-羧基和ε-胺基的氨基酸，其中ε-胺基与第一基团共价键合，α-羧基与第二基团共价键合。
• Filler for measuring enzyme activity, column packed with the filler, and method of measuring enzyme activity using the column
  申请人：SHOWA DENKO KABUSHIKI KAISHA

  公开号：EP0329190A2

  公开（公告）日：1989-08-23

  Enzyme activity is measured promptly with a high accuracy by introducing an enzyme, the activity of which is to be measured, into a column comprising a hollow tube packed with a filler comprising a support and a substrate that can be recognized by the enzyme, which is immobilized on the support, and measuring the amount of the obtained decomposition product of the substrate.

  酶的活性是通过将需要测量其活性的酶导入一个由空心管组成的柱中，空心管中填充物包括支撑物和可被固定在支撑物上的酶识别的底物，然后测量所获得的底物分解产物的量，从而快速、高精度地测量酶的活性。