(2S)-2-氨基-N-[(3R,4R,4aR,5R,6R)-3,4,4a,5,6,7-六氢-5,6,8-三羟基-3-甲基-1-氧代-1H-2-苯并吡喃-4-基]-丙酰胺 | 24397-89-5

• 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: (2S)-2-氨基-N-[(3R,4R,4aR,5R,6R)-3,4,4a,5,6,7-六氢-5,6,8-三羟基-3-甲基-1-氧代-1H-2-苯并吡喃-4-基]-丙酰胺
• 英文名称: Actinobolin
• 英文别名: (2S)-2-amino-N-[(3R,4R,4aR,5R,6R)-5,6,8-trihydroxy-3-methyl-1-oxo-3,4,4a,5,6,7-hexahydroisochromen-4-yl]propanamide
• CAS: 24397-89-5
• 化学式: C₁₃H₂₀N₂O₆
• 分子量: 300.31
• InChiKey: PQVQBAAWCOTEBG-NSVWQLETSA-N

物化性质

• 比旋光度：
  D28 +59° (c = 0.5 in pH 7 phosphate buffer)
• 沸点：
  441.54°C (rough estimate)
• 密度：
  1.2243 (rough estimate)

计算性质

• 辛醇/水分配系数(LogP)：
  -1.5
• 重原子数：
  21
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.69
• 拓扑面积：
  142
• 氢给体数：
  5
• 氢受体数：
  7

制备方法与用途

类别：有毒物品

• 毒性分级：中毒
• 急性毒性：
  • 腹腔注射-小鼠 LD50: 2884 毫克/公斤
  • 皮下注射-小鼠 LD50: 1828 毫克/公斤

可燃性危险特性：可燃；加热分解时释放有毒氮氧化物烟雾

储运特性：库房应保持通风、低温和干燥

灭火剂：干粉、泡沫、砂土、二氧化碳或雾状水

文献信息

• Multi-Layer Tablets and Bioadhesive Dosage Forms
  申请人：Nangia Avinash

  公开号：US20080311191A1

  公开（公告）日：2008-12-18

  Bioadhesives coatings increase the gastrointestinal retention time of orally-ingested medicaments. Certain bioadhesive coatings producing a fracture strength of at least 100 N/m 2 , as measured on rat intestine, when applied to at least one surface of a pharmaceutical dosage form for oral delivery of a drug, result in a gastrointestinal retention time of at least 4 hours in a fed beagle dog model, during which the drug is released from the dosage form. Multi-layer tablets, particularly those including hydrophobic excipients, are useful in administering hygroscopic and/or deliquescent drugs. In addition, varying the amount of drug in multi-layer tablets allows the release rate of the drug to be controlled.

  生物粘合剂涂层可以增加口服药物的胃肠道保留时间。当应用于至少一种药物剂型的表面以口服给药时，产生至少100 N/m²的断裂强度的某些生物粘合剂涂层（在大鼠肠道上测量）可导致在饲养的比格犬模型中至少保留4小时的胃肠道保留时间，在此期间药物从剂型中释放。多层片剂，特别是包括疏水助剂的多层片剂，可用于给予吸湿性和/或易溶性药物。此外，改变多层片剂中药物的量可以控制药物的释放速率。
• Oral formulations of medicaments
  申请人：Pfizer Limited

  公开号：EP1136067A1

  公开（公告）日：2001-09-26

  A formulation suitable for oral treatment with a medicament comprising: a solid masticable portion and one or more reservoir portions encompassed by said masticable portion; the solid masticable portion consisting of a fully edible material, having mechanical properties conducive to promoting mastication, typified by a stiffness measurement (i.e. Young's modulus) in the range of 0.01-5MPa, and compressive strength in the range of 10 to 10,000 mJ; the reservoir portion or portions comprising a releasable unit dose of the medicament in a fluid (preferably a liquid) form, with a viscosity below 800mPa.s at body temperature (ca. 36-ca.40°C), and preferably between the range of 50-200mPa.s; such that on mastication, the masticable portion is ruptured and the unit dose of the medicament is released in a short space of time from the reservoir portion into the oral cavity.

  一种适用于口服治疗的药物制剂，包括 固体可咀嚼部分和由所述可咀嚼部分包围的一个或多个储藏部分； 固体可咀嚼部分由完全可食用的材料组成，具有有利于促进咀嚼的机械性能，典型的刚度测量值（即杨氏模量）在0.01-5MPa之间，抗压强度在10-10,000 mJ之间； 储液器部分包括流体（最好是液体）形式的可释放单位剂量药物，在体温（约 36-约 40°C）下粘度低于 800mPa.s，最好在 50-200mPa.s 之间； 这样，在咀嚼时，可咀嚼部分破裂，单位剂量的药物在短时间内从储藏部分释放到口腔中。
• Vibrating oral care device
  申请人：The Gillette Company

  公开号：EP2008614A1

  公开（公告）日：2008-12-31

  A vibrating oral care device, including: a housing which can be gripped by human fingers; a battery within the housing; a flexible element having a long dimension, wherein the flexible element is releaseably secured into an end portion of the vibrating oral care device; an electric motor having an eccentric weight attached thereto for vibrating the flexible element; and a switch for electrically connecting the battery to the electric motor; wherein the flexible element further includes a rib that mates with the end portion of the vibrating oral care device to releaseably secure the flexible element to the vibrating oral care device.

  振动口腔护理装置，包括 可被人的手指握住的外壳 外壳内的电池 具有长尺寸的柔性元件，其中柔性元件可释放地固定在振动口腔护理装置的端部； 一个电动马达，其上有一个偏心重锤，用于振动柔性元件；以及 用于将电池与电动马达电连接的开关； 其中，柔性元件进一步包括与振动口腔护理装置的端部配合的肋条，以将柔性元件可释放地固定到振动口腔护理装置上。
• Processes and host cells for genome, pathway, and biomolecular engineering
  申请人：enEvolv, Inc.

  公开号：US10370654B2

  公开（公告）日：2019-08-06

  The present disclosure provides compositions and methods for genomic engineering.

  本公开提供了基因组工程的组合物和方法。
• Sustained-release matrices for dental application
  申请人：The Gillette Company, a Delaware corporation

  公开号：US20020081556A1

  公开（公告）日：2002-06-27

  A sustained-release matrix for dental application includes either an anti-microbial agent or a colorant that is released from the matrix when the matrix contacts water. The preferred matrices include a water-soluble polymer and a water-insoluble support resin.

  牙科用缓释基质包括抗微生物剂或着色剂，当基质与水接触时会从基质中释放出来。首选的基质包括水溶性聚合物和不溶于水的支撑树脂。