(2,5-Dioxopyrrolidin-1-yl) 2-formamidoacetate | 68385-27-3

• 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: (2,5-Dioxopyrrolidin-1-yl) 2-formamidoacetate
• CAS: 68385-27-3
• 化学式: C₇H₈N₂O₅
• 分子量: 200.151
• InChiKey: IRDDTBYIMIGMRR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.4
• 重原子数：
  14
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  92.8
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  L-谷氨酸-5-叔丁基酯 、 (2,5-Dioxopyrrolidin-1-yl) 2-formamidoacetate 在 碳酸氢钠 作用下， 以 四氢呋喃 、 水 为溶剂， 反应 16.0h， 以2.79 g的产率得到N-For-Gly-L-Glu(OtBu)-OH
  参考文献：
  名称：

  为细菌细胞中的核苷酸递送定制肽-核苷酸偶联物 (PNC)

  摘要：

  介绍了肽-2'-脱氧胸苷-5'-O-单磷酸结合物的设计和合成，作为核苷酸进入营养缺陷型大肠杆菌菌株的潜在活性传递系统。通过形成生物不稳定的化学连接，允许一系列寡肽与 5'-O-（二苄基磷酸酯）-2'-脱氧胸苷或其适当的 3'-衍生类似物反应，得到相关的肽-核苷酸加合物。使用基于正交保护和激活原理的策略，对接头和肽部分进行了合理的变化，以调整缀合物的代谢稳定性。

  DOI：

  10.1002/ejoc.201301781
• 作为产物：
  描述：

  N-羟基丁二酰亚胺 、 N-甲酰甘氨酸 在 N,N'-二环己基碳二亚胺 作用下， 以 四氢呋喃 为溶剂， 生成 (2,5-Dioxopyrrolidin-1-yl) 2-formamidoacetate
  参考文献：
  名称：

  为细菌细胞中的核苷酸递送定制肽-核苷酸偶联物 (PNC)

  摘要：

  介绍了肽-2'-脱氧胸苷-5'-O-单磷酸结合物的设计和合成，作为核苷酸进入营养缺陷型大肠杆菌菌株的潜在活性传递系统。通过形成生物不稳定的化学连接，允许一系列寡肽与 5'-O-（二苄基磷酸酯）-2'-脱氧胸苷或其适当的 3'-衍生类似物反应，得到相关的肽-核苷酸加合物。使用基于正交保护和激活原理的策略，对接头和肽部分进行了合理的变化，以调整缀合物的代谢稳定性。

  DOI：

  10.1002/ejoc.201301781

文献信息

• Lipid construct for delivery of insulin to a mammal
  申请人：SDG, INC.

  公开号：US10004686B2

  公开（公告）日：2018-06-26

  The instant invention is drawn to a hepatocyte targeted composition comprising insulin associated with a lipid construct comprising an amphipathic lipid and an extended amphipathic lipid that targets the construct to a receptor displayed by an hepatocyte. The composition can comprise a mixture of free insulin and insulin associated with the complex. The composition can be modified to protect insulin and the complex from degradation. The invention also includes methods for the manufacture of the composition and loading insulin into the composition and recycling various components of the composition. Methods of treating individuals inflicted with diabetes.

  本发明涉及一种肝细胞靶向组合物，该组合物包含与脂质构建物相关联的胰岛素，脂质构建物包括两性脂质和扩展两性脂质，该构建物可靶向肝细胞显示的受体。 该组合物可包括游离胰岛素和与复合物相关的胰岛素的混合物。 可以对组合物进行修饰，以保护胰岛素和复合物不被降解。 本发明还包括制造组合物、将胰岛素装入组合物以及回收组合物中各种成分的方法。 治疗糖尿病患者的方法。
• Orally bioavailable lipid-based constructs
  申请人：SDG, INC.

  公开号：US11517529B2

  公开（公告）日：2022-12-06

  The present invention is embodied by a composition capable of chaperoning a typically non-orally available therapeutic or diagnostic agent through the environment of the digestive tract such that the therapeutic or diagnostic agent is bioavailable. The composition may or may not be targeted to specific cellular receptors, such as hepatocytes. Therapeutic agents include, but are not limited to, insulin, calcitonin, serotonin, and other proteins. Targeting is accomplished with biotin or metal based targeting agents.

  本发明体现为一种组合物，它能够通过消化道环境对通常非口服的治疗剂或诊断剂进行陪衬，从而使治疗剂或诊断剂具有生物可利用性。该组合物可以针对或不针对特定的细胞受体，如肝细胞。治疗剂包括但不限于胰岛素、降钙素、血清素和其他蛋白质。生物素或金属靶向剂可实现靶向。
• Orally Bioavailable Lipid-Based Constructs
  申请人：Geho W. Blair

  公开号：US20100247625A1

  公开（公告）日：2010-09-30

  The present invention is embodied by a composition capable inducing weight loss in a patient in need thereof.
• HYDROPHILIC CHEMILUMINESCENT ACRIDINIUM LABELING REAGENTS
  申请人：Evangelista Ramon

  公开号：US20110014721A1

  公开（公告）日：2011-01-20

  In accordance with the present invention, it has been discovered that introduction of hydrophilic sulfoalkyl substituents and/or hydrophilic linkers derived from homocysteic acid, cysteic acid, glycine peptides, tetraethylene oxide, and the like, offset the hydrophobicity of the acridinium ring system to produce a more soluble label which can be attached to an antibody at higher loading before precipitation and aggregation problems are encountered. Additional compounds described herein contain linkers derived from short peptides and tetraethylene oxide which increase aqueous solubility due to hydrogen bonding with water molecules. The present invention also embraces reagents for multiple acridinium labeling for signal amplification composed of a peptide bearing several acridinium esters with sulfonate groups at regularly spaced intervals for increased solubility. The invention also embraces assays employing the above-described compounds.
• Lipid Construct for Delivery of Insulin to a Mammal
  申请人：SDG, INC.

  公开号：US20130267462A1

  公开（公告）日：2013-10-10

  The instant invention is drawn to a hepatocyte targeted composition comprising insulin associated with a lipid construct comprising an amphipathic lipid and an extended amphipathic lipid that targets the construct to a receptor displayed by an hepatocyte. The composition can comprise a mixture of free insulin and insulin associated with the complex. The composition can be modified to protect insulin and the complex from degradation. The invention also includes methods for the manufacture of the composition and loading insulin into the composition and recycling various components of the composition. Methods of treating individuals inflicted with diabetes.