(2S)-2-azaniumyl-5-(naphthalene-1-carbonylamino)-5-oxopentanoate

• 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: (2S)-2-azaniumyl-5-(naphthalene-1-carbonylamino)-5-oxopentanoate
• 化学式: C16H16N2O4
• 分子量: 300.31
• InChiKey: HBFLDCKOTCDLJS-ZDUSSCGKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.1
• 重原子数：
  22
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  110
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• [EN] TARGETED NOTCH PATHWAY INHIBITORS<br/>[FR] INHIBITEURS DE LA VOIE DE NOTCH CIBLÉE
  申请人：HOFFMANN LA ROCHE

  公开号：WO2016198366A1

  公开（公告）日：2016-12-15

  The instant invention relates to novel conjugates of formula (I): S - L - A (I) or salts thereof, wherein A is a gamma-secretase inhibitor, L is a linker and S is a peptidase-specific substrate, as well as processes for their manufacture, pharmaceutical compositions comprising them, and their use as medicaments, especially for the treatment of renal diseases and tissue damage in the kidney.

  本发明涉及式(I)的新型共轭物：S - L - A (I)或其盐，其中A为γ-分泌酶抑制剂，L为连接子，S为肽酶特异性底物，以及它们的制备方法、包含它们的药物组合物及其作为药物，特别是用于治疗肾脏疾病和肾脏组织损伤的用途。
• Microorganisms detection methods and the separation of agglutinated microorganisms, and a kit for use therein
  申请人：E-Y LABORATORIES, INC.

  公开号：EP0122023A1

  公开（公告）日：1984-10-17

  A test for the differential detection of suspected N. gonorrhoeae (N.g.) and N. meningitidis (N.m.) in provided by contacting a suspected sample with a lectin, preferably wheat germ agglutinin and either soy bean agglutinin or STA potato lectin. An agglutinin reaction is a positive indication of the presence of such microorganisms. Separate portions of the specimen may be contaced with fast substrates specific for (a) N.g., (b) N.m., and (c) B. catarrhalis. Suitable fast substrates are proline naphthylamide, gamma glutamyl naphthylamide, and glycyl prolyl naphthylamide, respectively, each substituted with an electron donating group at the 4-position, 6-position, or both. Another portion of the specimen may be reacted with a substrate for beta-galactosidase enzyme, a positive reaction being an indication that the specimen contains N.lactimica. Autoagglutination, which could otherwise give a false positive in the lectin test, may be prevented by pretreatment of the specimen with DNA'ase and/or an anhydride such as succinic anhydride.

  一种用于鉴别检测疑似淋球菌（N.g.）和脑膜炎双球菌（N.m.）的检测方法是将疑似样本与凝集素（最好是小麦胚芽凝集素和大豆凝集素或 STA 马铃薯凝集素）接触。凝集素反应是此类微生物存在的阳性指标。标本的不同部分可分别与(a) N.g.、(b) N.m.和(c) B. catarrhalis 的特异性快速底物反应。合适的快速底物分别是脯氨酸萘甲酰胺、γ-谷氨酰萘甲酰胺和甘氨酰脯氨酰萘甲酰胺，每种底物都在 4 位、6 位或两者上被电子捐赠基团取代。标本的另一部分可与β-半乳糖苷酶的底物反应，阳性反应表明标本中含有乳酸奈米卡氏菌。用 DNA'ase 和/或酸酐（如琥珀酸酐）对标本进行预处理，可防止自身凝集，否则会在凝集素检测中出现假阳性。
• Colorimetric assay for enzymes, diagnostic article therefor and a method for forming such article
  申请人：E-Y LABORATORIES, INC.

  公开号：EP0122028A1

  公开（公告）日：1984-10-17

  A method for the colorimetric assay of a suspected enzyme-containing substance in a biologically derived specimen is provided by absorbing a substrate for the enzyme onto an absorbent surface such as a swab, which is contacted with the specimen to produce a color if the enzyme is present. Multiple substrates producing different colors may be absorbed onto the swab for the detection of multiple enzymes. The invention includes a diagnostic article, and its formation, incorporating this principle.

  提供了一种对生物样本中可疑含酶物质进行比色检测的方法，该方法是将酶的底物吸附在吸附表面（如拭子）上，拭子与样本接触后，如果存在酶，就会产生颜色。可将多种产生不同颜色的底物吸收到拭子上，以检测多种酶。本发明包括包含这一原理的诊断物品及其形成。
• Reagents for assay of gamma-glutamyl-transpeptidase
  申请人：UNITIKA LTD.

  公开号：EP0266905A1

  公开（公告）日：1988-05-11

  A reagent for assaying γ-glutamyltranspeptidase (γ-GTP) which contains an amino acid dehydrogenase and a substrate specific to γ-glutamyltranspeptidase activity. The reagent can be used to assay the γ-GTP activity directly from the continuous course of reaction without using a standard substance with known activity. The procedure required is simple and easy, and the reagent is capable of determining γ-GTP activity with good accuracy and without affecting by interfering substances, making it satisfactory for routine use in clinical laboratories.

  一种用于测定γ-谷氨酰转肽酶（γ-GTP）的试剂，它含有氨基酸脱氢酶和对γ-谷氨酰转肽酶活性有特异性的底物。该试剂无需使用已知活性的标准物质，即可直接从连续反应过程中检测 γ-GTP 活性。该试剂所需的步骤简单易行，能够准确测定 γ-GTP 活性，且不受干扰物质的影响，因此非常适合临床实验室的常规使用。
• Novel amino acid substituted 4-aminophenazones for measuring enzyme activity
  申请人：THE BOARD OF GOVERNORS OF WAYNE STATE UNIVERSITY

  公开号：EP0346870A2

  公开（公告）日：1989-12-20

  Novel substrates which are amino acid 4-amino phenazones for detecting enzymes, particularly L-gamma-glutamyltransferase, are described. The amino acid gamma-glutamyl-4-aminophenazone reacts with the enzyme to produce 4-aminophenazone which is an amino dye intermediate. The amino dye intermediate is coupled with a second dye intermediate to form a chromogen. The 4-aminophenazone is particularly reacted with a phenolic naphtholic or aniline compound, particularly the phenolic compound 2-hydroxy-3,5-dichlorobenzenesulfonate, to form a red chromogen in the presence of an oxidizing agent, such as bilirubin oxidase.

  描述了用于检测酶，特别是 L-γ-谷氨酰转移酶的氨基酸 4-氨基酚氮酮新型底物。氨基酸γ-谷氨酰-4-氨基酚氮酮与酶反应生成 4-氨基酚氮酮，它是一种氨基染料中间体。氨基染料中间体与第二种染料中间体偶联形成发色剂。4-aminophenazone 与酚类萘化合物或苯胺化合物，特别是酚类化合物 2-羟基-3,5-二氯苯磺酸盐反应，在氧化剂（如胆红素氧化酶）存在下形成红色发色剂。