4-甲基伞形酮-2-乙酸胺基-2-脱氧-Α-D-吡喃葡糖苷 | 80265-04-9

• 物质功能分类: 生物化工 - 糖类化合物 - 单糖
• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 香豆素及其衍生物
• 中文名称: 4-甲基伞形酮-2-乙酸胺基-2-脱氧-Α-D-吡喃葡糖苷
• 中文别名: 4-甲基伞形基-2-乙酰氨基-2-脱氧-Α-D-葡萄糖苷；4-甲基伞形酮-2-乙酰胺基-2-脱氧-Alpha-D-吡喃葡萄糖苷；4-甲基伞形酮-2-乙酰胺基-2-脱氧-α-D-吡喃葡萄糖苷
• 英文名称: 4-methylumbelliferyl 2-acetamido-2-deoxy-α-D-glucopyranoside
• 英文别名: 4-methylumbelliferyl-N-acetyl-α-D-glucosaminide；4-Methylumbelliferyl-N-acetyl-alpha-D-glucosaminide；4-Methylumbelliferyl-2-acetamido-2-deoxy-alpha-D-glucopyranoside；N-[(2R,3R,4R,5S,6R)-4,5-dihydroxy-6-(hydroxymethyl)-2-(4-methyl-2-oxochromen-7-yl)oxyoxan-3-yl]acetamide
• CAS: 80265-04-9
• 化学式: C₁₈H₂₁NO₈
• 分子量: 379.367
• InChiKey: QCTHLCFVVACBSA-FGTAOJJYSA-N

物化性质

• 熔点：
  224-225°C
• 沸点：
  732.2±60.0 °C(Predicted)
• 密度：
  1.47±0.1 g/cm3(Predicted)
• 溶解度：
  DMSO（微溶）、甲醇（微溶）、水（微溶、加热）

计算性质

• 辛醇/水分配系数(LogP)：
  -0.8
• 重原子数：
  27
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  135
• 氢给体数：
  4
• 氢受体数：
  8

安全信息

• 危险品标志：
  Xi
• 安全说明：
  S22,S26,S36
• 危险类别码：
  R36/37/38
• 海关编码：
  29389090
• 储存条件：
  -20°C

制备方法与用途

4-甲基伞形花序基-N-乙酰基-α-D-氨基葡萄糖苷是一种用于检测α-N-酰基氨基葡萄糖苷酶的荧光底物。

反应信息

• 作为反应物：
  描述：

  4-甲基伞形酮-2-乙酸胺基-2-脱氧-Α-D-吡喃葡糖苷 在 盐酸 、 乙酸酐 、 potassium hydrogencarbonate 作用下， 生成 D-GlcNAc
  参考文献：
  名称：

  4-Methylumbelliferyl 2-acetamido-2-deoxy-α-d-glucopyranoside, a fluorogenic substrate for N-acetyl-α-D-glucos-aminidase

  摘要：

  Condensation of dimeric 3,4,6-tri-O-acetyl-2-deoxy-2-nitroso-alpha-D-glucopyranosyl chloride with 4-methylumbelliferone gave crystalline 4-methylumbelliferyl 3,4,6-tri-O-acetyl-2-deoxy-2-oximino-alpha-D-arabino-hexopyranoside. Acetylation of this adduct, reduction of the resulting crude O-acetyloxime with borane in oxolane, and acetylation gave the 3,4,6-tri-O-acetyl derivative of 4-methylumbelliferyl 2-acetamido-2-deoxy-alpha-D-glucopyranoside (1). A new sensitive assay of N-acetyl-alpha-D-glucosaminidase (EC 3.2.1.50) is made possible by fluorometric measurement of 4-methylumbelliferone liberated by enzymic hydrolysis of glycoside 1. Such assays are illustrated by results obtained with enzyme preparations from pig liver and human-blood serum.

  DOI：

  10.1016/s0008-6215(00)84698-4
• 作为产物：
  描述：

  4-methylumbelliferyl 2-acetamido-3,4,6-tri-O-acetyl-2-deoxy-α-D-glucopyranoside 在 sodium methylate 作用下， 以 甲醇 、 氯仿 为溶剂， 反应 0.05h， 以75%的产率得到4-甲基伞形酮-2-乙酸胺基-2-脱氧-Α-D-吡喃葡糖苷
  参考文献：
  名称：

  4-Methylumbelliferyl 2-acetamido-2-deoxy-α-d-glucopyranoside, a fluorogenic substrate for N-acetyl-α-D-glucos-aminidase

  摘要：

  Condensation of dimeric 3,4,6-tri-O-acetyl-2-deoxy-2-nitroso-alpha-D-glucopyranosyl chloride with 4-methylumbelliferone gave crystalline 4-methylumbelliferyl 3,4,6-tri-O-acetyl-2-deoxy-2-oximino-alpha-D-arabino-hexopyranoside. Acetylation of this adduct, reduction of the resulting crude O-acetyloxime with borane in oxolane, and acetylation gave the 3,4,6-tri-O-acetyl derivative of 4-methylumbelliferyl 2-acetamido-2-deoxy-alpha-D-glucopyranoside (1). A new sensitive assay of N-acetyl-alpha-D-glucosaminidase (EC 3.2.1.50) is made possible by fluorometric measurement of 4-methylumbelliferone liberated by enzymic hydrolysis of glycoside 1. Such assays are illustrated by results obtained with enzyme preparations from pig liver and human-blood serum.

  DOI：

  10.1016/s0008-6215(00)84698-4

文献信息

• Präparat zur Wirkstoffapplikation in Kleinsttröpfchenform
  申请人：Cevc, Gregor, Prof. Dr.

  公开号：EP0475160A1

  公开（公告）日：1992-03-18

  Die Erfindung betrifft ein Präparat zur Applikation von Wirkstoffen in Form kleinster, insbesondere mit einer membranartigen Hülle aus einer oder wenigen Lagen amphiphiler Moleküle bzw. mit einer amphiphilen Trägersubstanz versehenen Flüssigkeitströpfchen, insbesondere zum Transport des Wirkstoffes in und durch natürliche Barrieren und Konstriktionen wie Häute und dergleichen. Das Präparat weist einen Gehalt einer randaktiven Substanz auf, der bis zu 99 Mol.-% des Gehaltes dieser Substanz entspricht, durch den der Solubilisierungspunkt der Tröpfchen erreicht wird. Das Präparat eignet sich zur nichtinvasiven Verabreichung von Antidiabetica, insbesondere von Insulin. Die Erfindung betrifft außerdem ein Verfahren zur Herstellung solcher Präparate.

  本发明涉及一种以微小液滴形式施用活性物质的制剂，特别是具有一层或几层两亲性分子或两亲性载体物质的膜状包膜，尤其是用于将活性物质输送到或通过皮肤等天然屏障和收缩物。制剂中边缘活性物质的含量最高可达 99 摩尔%，从而达到液滴的溶解点。该制剂适用于非侵入性给药抗糖尿病药物，特别是胰岛素。本发明还涉及生产这种制剂的工艺。
• METHOD TO READ BIOLOGICAL INDICATOR
  申请人：Ethicon, Inc.

  公开号：EP3366315A1

  公开（公告）日：2018-08-29

  A method for detecting biological activity in a biological indicator comprises the steps of providing a known quantity of spores containing a fixed number of copies of an enzyme and a liquid growth medium comprising substrates of the enzyme. The enzyme substrates have a first emission spectrum, and are configured to be converted by the enzyme to substrate derivatives having a second emission spectrum. The spores are exposed to the liquid growth medium, and the liquid growth medium is measured for the second emission spectrum, and either no change in the second emission spectrum or a linear increase in the second emission spectrum, is detected as a function of time.

  一种检测生物指示剂中生物活性的方法包括以下步骤：提供已知数量的孢子，其中含有固定拷贝数的酶和含有酶底物的液体生长培养基。酶底物具有第一发射光谱，并可被酶转化为具有第二发射光谱的底物衍生物。孢子暴露在液体生长介质中，测量液体生长介质的第二发射光谱，检测第二发射光谱随时间的变化是无变化还是线性增加。
• SYSTEMS AND METHODS FOR CONFIRMING ACTIVATION OF BIOLOGICAL INDICATORS
  申请人：Ethicon, Inc.

  公开号：EP3421056A1

  公开（公告）日：2019-01-02

  Biological indicators may be improperly activated. The disclosed subject matter is directed to methods of confirming that a biological indicator having an ampule containing a growth medium has been properly activated such that it may be assayed. The methods may include the steps of measuring a first fluorescence intensity of the biological indicator, heating the biological indicator; quenching the fluorescence intensity of the biological indicator from the first fluorescence intensity to a second fluorescence intensity, measuring the second fluorescence intensity; comparing the second fluorescence intensity and first fluorescence intensity to obtain a comparison value; and determining that the comparison value corresponds to a quenching metric of the liquid growth medium.

  生物指示剂可能会被不适当地激活。所公开的主题涉及确认生物指示剂的方法，该生物指示剂有一个含有生长培养基的安瓿，已被适当活化，可以对其进行检测。这些方法可包括以下步骤：测量生物指示剂的第一荧光强度，加热生物指示剂；将生物指示剂的荧光强度从第一荧光强度淬灭至第二荧光强度，测量第二荧光强度；比较第二荧光强度和第一荧光强度以获得比较值；以及确定比较值对应于液体生长介质的淬灭指标。
• NOVEL ANTI-HUMAN TRANSFERRIN RECEPTOR ANTIBODY CAPABLE OF PENETRATING BLOOD-BRAIN BARRIER
  申请人：JCR Pharmaceuticals Co., Ltd.

  公开号：EP3560958A1

  公开（公告）日：2019-10-30

  Provided is an anti-human transferrin receptor antibody or an analog thereof, wherein in the heavy chain variable region of the antibody, (a) CDR1 comprises the amino acid sequence set forth as SEQ ID NO: 62 or SEQ ID NO: 63, (b) CDR2 comprises the amino acid sequence set forth as SEQ ID NO: 13 or SEQ ID NO: 14, and (c) CDR3 comprises the amino acid sequence set forth as SEQ ID NO: 15 or SEQ ID NO: 16, and an analogue thereof.

  提供了一种抗人转铁蛋白受体抗体或其类似物，其中在抗体的重链可变区中，(a) CDR1 包括 SEQ ID NO: 62 或 SEQ ID NO: 63 所列的氨基酸序列，(b) CDR2 包括 SEQ ID NO: 13 或 SEQ ID NO: 14 所列的氨基酸序列，以及(c) CDR3 包括 SEQ ID NO: 15 或 SEQ ID NO: 16 所列的氨基酸序列及其类似物。
• Biological indicator
  申请人：American Sterilizer Company

  公开号：US10011843B2

  公开（公告）日：2018-07-03

  This invention relates to a biological indicator derived from a composition comprising: a host organism comprising a spore forming bacteria; a reporter gene for producing an indicator enzyme; a regulatory gene; and a vehicle for inserting the reporter gene and the regulatory gene in the host organism; the host organism bearing a transposable genetic element in its genome for inserting an insertion sequence in the regulatory gene; the insertion sequence comprising a transposase, a pair of terminal inverted repeat sequences, and at least one open reading frame for expressing the transposase. The vehicle may be taken up by the host organism. The insertion sequence may be inserted in the regulatory gene. The host organism may undergo sporulation to form the biological indicator. A process and an apparatus for using the biological indicator are disclosed.

  本发明涉及一种生物指示剂，其成分包括：由形成孢子的细菌组成的宿主生物；产生指示剂酶的报告基因；调控基因；以及将报告基因和调控基因插入宿主生物的载体；宿主生物的基因组中含有转座遗传因子，用于在调控基因中插入插入序列；插入序列包括转座酶、一对末端倒置重复序列和至少一个用于表达转座酶的开放阅读框。载体可被宿主生物吸收。插入序列可插入调控基因中。宿主生物可进行孢子繁殖以形成生物指示剂。本发明公开了一种使用生物指示剂的工艺和装置。