二氨基生物素 | 22342-46-7

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 脂肪酰基
• 中文名称: 二氨基生物素
• 中文别名: 生物素杂质
• 英文名称: diaminobiotin
• 英文别名: biotin；cis-diamino biotin；(2S,3S,4R)-cis-5-(3,4-diaminotetrahydro-2-thienyl)valeric acid；5-((2S)-3c,4c-diamino-tetrahydro-[2r]thienyl)-valeric acid；5-((2S)-3c,4c-Diamino-tetrahydro-[2r]thienyl)-valeriansaeure；5-[(2S,3S,4R)-3,4-diaminothiolan-2-yl]pentanoic acid
• CAS: 22342-46-7
• 化学式: C₉H₁₈N₂O₂S
• 分子量: 218.32
• InChiKey: JKNCSZDPWAVQAI-ZKWXMUAHSA-N

物化性质

• 熔点：
  >175°C (dec.)
• 溶解度：
  H2O：20 mg/mL，澄清，无色

计算性质

• 辛醇/水分配系数(LogP)：
  -2.7
• 重原子数：
  14
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.89
• 拓扑面积：
  115
• 氢给体数：
  3
• 氢受体数：
  5

安全信息

• 海关编码：
  2934999090

反应信息

• 作为反应物：
  描述：

  二氨基生物素 在 L-精氨酸 、 potassium carbonate 作用下， 生成 D-生物素
  参考文献：
  名称：

  生物素 生物素和表皮球蛋白的合成。

  摘要：

  DOI：

  10.1021/jo01165a023
• 作为产物：
  描述：

  (+/-)-5-(2-oxo-1-phenylcarbamoyl-(3ar,6ac)-hexahydro-thieno[3,4-d]imidazol-4t-yl)-valeric acid anilide 在 甲醇 、 barium dihydroxide 作用下， 生成 二氨基生物素
  参考文献：
  名称：

  生物素 生物素和表皮球蛋白的合成。

  摘要：

  DOI：

  10.1021/jo01165a023

文献信息

• Cyclosporin derivatives
  申请人：Fischer Gunter

  公开号：US09453051B2

  公开（公告）日：2016-09-27

  The present invention relates to novel cyclosporin derivatives that do not cross the cellular membrane. The compounds according to the invention are used in medicine, more particularly in the treatment/diagnosis of acute and chronic inflammatory diseases, viral infections, cancer, degenerative muscle diseases, neurodegenerative diseases and damage that is associated with calcium homeostasis impairment. The novel cyclosporin derivatives additionally have no immunosuppressive effect.

  本发明涉及不穿过细胞膜的新型环孢素衍生物。根据本发明的化合物用于医药，特别是在治疗/诊断急性及慢性炎症疾病、病毒感染、癌症、退行性肌肉疾病、神经退行性疾病以及与钙稳态受损相关的损害。这些新型环孢素衍生物另外不具有免疫抑制作用。
• [EN] NOVEL KLK4 INHIBITORS<br/>[FR] NOUVEAUX INHIBITEURS DE KLK4
  申请人：UNIV ANTWERPEN

  公开号：WO2015144933A1

  公开（公告）日：2015-10-01

  The present invention relates to novel compounds and probes which have a common chemical structure necessary to obtain potent inhibitory activity against KLK4 and/or may be used for the detection of KLK4 peptides and their activity. It further relates to the use of these compounds and methods for inhibiting and/or detecting KLK4 activity in vitro and in vivo by making use of said probes or inhibitors. The compounds of the invention differ from prior art compounds at least in the presence of phenyl guanidine (instead of e.g. benzyl guanidine) and/or the presence of a heteroatom in the tail group, their combined presence unexpectedly leading to potent and selective KLK4 inhibitory activity.

  本发明涉及具有共同化学结构的新化合物和探针，这种结构对于获得强大的对KLK4的抑制活性是必要的，或者可用于检测KLK4肽及其活性。它进一步涉及利用这些化合物和方法通过利用所述的探针或抑制剂来抑制和/或检测体外和体内的KLK4活性。本发明的化合物与先前的化合物不同，至少在于存在苯基胍（而不是苄基胍等）和/或尾基中存在杂原子，它们的共同存在意外地导致强大和选择性的KLK4抑制活性。
• 一种苄基生物素脱苄制备生物素的方法
  申请人：菏泽市方明制药有限公司

  公开号：CN103788112B

  公开（公告）日：2016-03-09

  本发明属于精细化工技术领域，公开了一种苄基生物素脱苄制备生物素的方法，包括以下过程：将不同方法合成的二苄基生物素在分散剂协助下充分分散在氢溴酸中，快速搅拌、加热蒸馏，将蒸出的溴化苄和氢溴酸冷凝、分液，上层的氢溴酸回流到反应液，下层的溴化苄分出，反应结束，快速降温，真空蒸馏回收氢溴酸，残余固体加入定量的水或母液升温溶解，调节酸碱度后，加活性炭脱色，降温析出生物素结晶（理论量的87%），溴化苄经干燥、蒸馏提纯，得合格的溴化苄，结晶母液中残余的开环物，在母液连续套用20次后，液碱控制PH值，三光气关环得回收生物素，可平均提高5%的收率。本工艺安全环保，收率高、质量好、费用低，适用于工业化生产。
• HALOGENATED BIOTIN-MODIFIED DIMER AND USE THEREOF
  申请人：The University of Tokyo

  公开号：US20210214376A1

  公开（公告）日：2021-07-15

  An object of the present invention is to provide a halogenated biotin-modified dimer, which is capable of imaging diagnosis or treatment by labeling with a halogen, a biotin-modified dimer having a high affinity for a mutant streptavidin with a low affinity for natural biotin. The present invention provides a compound represented by the following formula (1) or a salt thereof: wherein the meaning of each symbol is the same as that described in the specification.

  本发明的目的是提供一种卤代生物素修饰二聚体，该二聚体能够通过标记卤素进行成像诊断或治疗，并具有高亲和力的突变链霉亲和素和低亲和力的天然生物素。本发明提供了以下式（1）所表示的化合物或其盐：其中每个符号的含义与说明书中描述的相同。
• Imaging Biotin Trafficking In Vivo with Positron Emission Tomography
  作者：Salvatore Bongarzone、Teresa Sementa、Joel Dunn、Jayanta Bordoloi、Kavitha Sunassee、Philip J. Blower、Antony Gee

  DOI：10.1021/acs.jmedchem.0c00494

  日期：2020.8.13

  The water-soluble vitamin biotin is essential for cellular growth, development, and well-being, but its absorption, distribution, metabolism, and excretion are poorly understood. This paper describes the radiolabeling of biotin with the positron emission tomography (PET) radionuclide carbon-11 (C-11]biotin) to enable the quantitative study of biotin trafficking in vivo. We show that intravenously administered [C-11]biotin is quickly distributed to the liver, kidneys, retina, heart, and brain in rodents-consistent with the known expression of the biotin transporter-and there is a surprising accumulation in the brown adipose tissue (BAT). Orally administered [C-11]biotin was rapidly absorbed in the small intestine and swiftly distributed to the same organs. Preadministration of nonradioactive biotin inhibited organ uptake and increased excretion. [C-11]Biotin PET imaging therefore provides a dynamic in vivo map of transporter-mediated biotin trafficking in healthy rodents. This technique will enable the exploration of biotin trafficking in humans and its use as a research tool for diagnostic imaging of obesity/diabetes, bacterial infection, and cancer.