isovaleryl-Val-Val-Sta(3xi,4xi)-Ala-Sta(3xi,4xi)-OH

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 肽模拟物
• 英文名称: isovaleryl-Val-Val-Sta(3xi,4xi)-Ala-Sta(3xi,4xi)-OH
• 英文别名: 3-hydroxy-4-[[(2S)-2-[[3-hydroxy-6-methyl-4-[[(2S)-3-methyl-2-[[(2S)-3-methyl-2-(3-methylbutanoylamino)butanoyl]amino]butanoyl]amino]heptanoyl]amino]propanoyl]amino]-6-methylheptanoic acid
• 化学式: C₃₄H₆₃N₅O₉
• 分子量: 685.9
• InChiKey: FAXGPCHRFPCXOO-JHTFMCFMSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  48
• 可旋转键数：
  22
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.82
• 拓扑面积：
  223
• 氢给体数：
  8
• 氢受体数：
  9

文献信息

• Process for preparing schiff base adducts of amines with o-hydroxy aldehydes and compositions of matter based thereon
  申请人：——

  公开号：US20030125528A1

  公开（公告）日：2003-07-03

  An improved process is described for preparing Schiff base condensation adduct final products whose components comprise a protein having beneficial activity in animals, and an aromatic o-hydroxy aldehyde, which comprises bringing together the above-mentioned components in an aqueous environment at a pH of 7.0 or higher to form a reaction mixture, under conditions effective to drive said condensation reaction substantially to completion by removing from about 97.0% to about 99.9% by weight, preferably from about 98.0% to about 99.0% by weight of the water already present or produced during said condensation reaction, consistent with maintaining the integrity of the condensation reactants and adduct final product, and to assure a rate of conversion to said condensation adduct final product, i.e., with resulting yield of said condensation adduct final product of equal to or greater than about 98.5% by weight, preferably equal to or greater than about 99.5% by weight based on the weight of the reactants. Preferred aromatic o-hydroxy aldehydes comprise o-vanillin; salicylaldehyde; 2,3-dihydroxybenzaldehyde; 2,6-dihydroxybenz-aldehyde; 2-hydroxy-3-ethoxybenzaldehyde; or pyridoxal. A very wide range of proteins may be employed. The improved process provides yields over 90% and substantially quantitative conversion of the aldehyde and protein to the condensation adduct.

  本文描述了一种改进的方法，用于制备Schiff碱缩合加合物的最终产物，其组分包括在动物中具有有益活性的蛋白质和芳香族o-羟基醛。该方法包括在pH为7.0或更高的水环境中将上述组分结合在一起以形成反应混合物，通过有效的条件将缩合反应驱动到几乎完成，其中从已有的水分中或在缩合反应期间产生的水分中除去大约97.0%到99.9%的重量，最好是从98.0%到99.0%的重量，保持缩合反应物和加合物最终产物的完整性，并确保转化为所述缩合加合物最终产物的速率，即所得缩合加合物最终产物的产率等于或大于约98.5%的重量，最好等于或大于约99.5%的重量，基于反应物的重量。首选的芳香族o-羟基醛包括邻香草醛；水杨醛；2,3-二羟基苯甲醛；2,6-二羟基苯甲醛；2-羟基-3-乙氧基苯甲醛；或吡哆醛。可以使用非常广泛的蛋白质。改进的方法提供了超过90%的产率和几乎定量的醛和蛋白质转化为缩合加合物。
• Pharmaceutical compositions for the treatment of thrombosis
  申请人：DENDREON CORPORATION

  公开号：EP1772516A1

  公开（公告）日：2007-04-11

  Proteins which have activity as anticoagulants and/or serine protease inhibitors and have at least one NAP domain are described. Certain of these proteins have factor Xa inhibitory activity and others have activity as inhibitors of factor VIIa/TF. These proteins can be isolated from natural sources as nematodes, chemically synthesized or made by recombinant methods using various DNA expression systems.

  本文介绍了具有抗凝剂和/或丝氨酸蛋白酶抑制剂活性并至少有一个 NAP 结构域的蛋白质。其中某些蛋白质具有 Xa 因子抑制活性，另一些则具有 VIIa/TF 因子抑制活性。这些蛋白质可以从线虫等天然来源中分离出来，也可以通过化学合成或使用各种 DNA 表达系统的重组方法制成。
• PHARMACEUTICAL COMPOSITIONS COMPRISING A TUNGSTEN SALT (VI) FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS, PARTICULARLY ALZHEIMER'S DISEASE AND SCHIZOPHRENIA
  申请人：Universidad de Barcelona

  公开号：EP1972342A1

  公开（公告）日：2008-09-24

  Pharmaceutical compositions comprising an effective amount of a tungsten (VI) compound, preferably of a tungstate salt, and more preferably of sodium tungstate (Na2WO4), are useful for the prophylactic and/or therapeutical treatment of neurodegenerative disorders in a mammal, including a human, in particular, for the prophylactic and/or therapeutical treatment of Alzheimer's disease or schizophrenia. The effect of sodium tungstate dihydrate on the phosphorylation of tau in a model of rat insulin resistance and in a model of type-1 diabetes has been assessed. The therapeutic treatment of tauopathies that derives from this invention involves several advantages: it targets a GSK3; specificity since it reduces the abnormal hyperphosphorylation of a neural specific protein, tau, efficacy, lack of toxicity, and low price.

  包含有效量的钨（VI）化合物，优选钨酸盐，更优选钨酸钠（Na2WO4）的药物组合物，可用于包括人类在内的哺乳动物神经退行性疾病的预防和/或治疗，特别是阿尔茨海默病或精神分裂症的预防和/或治疗。已经评估了钨酸钠二水合物在大鼠胰岛素抵抗模型和 1 型糖尿病模型中对 tau 磷酸化的影响。本发明对tau病的治疗具有以下几个优点：以GSK3为靶点；特异性，因为它能减少神经特异蛋白tau的异常过度磷酸化；疗效好；无毒性；价格低廉。
• Sampling systems and related materials and methods
  申请人：Progenity Inc.

  公开号：US10588608B2

  公开（公告）日：2020-03-17

  Sampling systems that include an absorbent material a preservative, such as an analyte preservative, as well as related materials and methods, are disclosed.

  本文公开了包括吸收材料和防腐剂（如分析防腐剂）的取样系统，以及相关材料和方法。
• Gastrointestinal tract detection methods, devices and systems
  申请人：Progenity Inc.

  公开号：US10610104B2

  公开（公告）日：2020-04-07

  The present disclosure relates to gastrointestinal (GI) tract detection methods, devices and systems.

  本公开涉及胃肠道（GI）检测方法、装置和系统。