1-(4-aminobutyl)-1H-pyrrolyl-2,5-dione | 945530-68-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: 1-(4-aminobutyl)-1H-pyrrolyl-2,5-dione
• 英文别名: 4-maleimido-1-butanamine；1-(4-aminobutyl)-2,5-dihydro-1H-pyrrole-2,5-dione；N-(4-aminobutyl)maleimide；1-(4-aminobutyl)pyrrole-2,5-dione
• CAS: 945530-68-7
• 化学式: C₈H₁₂N₂O₂
• 分子量: 168.195
• InChiKey: PBDFRUDGHBFXII-UHFFFAOYSA-N

物化性质

• 沸点：
  309.1±25.0 °C(Predicted)
• 密度：
  1.198±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  12
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  63.4
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-(4-aminobutyl)-1H-pyrrolyl-2,5-dione 在 N,N-二异丙基乙胺 作用下， 以 乙酸乙酯 、 N,N-二甲基甲酰胺 为溶剂， 生成 2-chloro-6-(4-maleimidobutanecarboxamido)resorufin
  参考文献：
  名称：

  INTRACELLULAR ORGANELLE PEPTIDE TARGETED ENZYME SUBSTRATES

  摘要：

  该发明涉及基于细胞器酶活性的底物和方法，用于可视化细胞内细胞器，如溶酶体、过氧化物酶体、细胞核、内质网和高尔基体。这些化合物代表了具有化学上不同的酶底物与靶向和检测底物的新型组合，这些底物受到靶细胞器内的酶活性的激活而产生可检测信号。该发明的细胞器靶向酶底物旨在在一些细胞器中发现的较低pH值下提供高荧光，并可用于监测细胞内酶活性的非常低浓度。

  公开号：

  US20150219654A1
• 作为产物：
  描述：

  (Z)-4-((4-((tert-butoxycarbonyl)amino)butyl)amino)-4-oxobut-2-enoic acid 在 sodium acetate 、 乙酸酐 、 苯甲醚 、 三氟乙酸 作用下， 以 丙酮 为溶剂， 反应 2.0h， 生成 1-(4-aminobutyl)-1H-pyrrolyl-2,5-dione
  参考文献：
  名称：

  Synthesis and characterization of a new polymer–drug conjugate with pH-induced activity

  摘要：

  A well-defined, stimuli-responsive tetrapolymer with pH-responsive characteristics and targeting specificity has been synthesized by radical copolymerization of methacrylic acid. N-(2-hydroxypropyl)methacrylamide, methacryloyl glycylglycyl sulfamethoxazole, and N-(methacryloyl)glycylglycine 4-nitrophenyl ester. The structure and properties of tetrapolymer were investigated by NMR, FT-IR, UV-visible absorption, TEM and gel permeation chromatography. Incorporation of maleimide linker into tetrapolymer facilitates its conjugation with antibody fragments, as demonstrated by the solid-phase immunoassay experiments. The TEM image shows that tetrapolymer had self-assembled a spherical micelle with a diameter ranging from 50 to 150 nm. Altering the pH of the solution leads to a different extent of aggregation at pH 6.5-3.5, responding in accordance with the properties associated with the extracellular environment of solid tumors and endocytosis. Furthermore, fluorescence spectroscopy indicated a critical micelle concentration (CMC) of 1 mg/mL. Because of the solvation and ionization effects, the tetrapolymer showed considerably enhanced antibacterial activities against Escherichia coli in the presence of DMSO and the antibacterial activity increased with decreasing pH value. (C) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.polymer.2012.06.006

文献信息

• [EN] ADHESIVE PHOTOPROTECTIVE COMPOUNDS AND USES THEREOF<br/>[FR] COMPOSÉS PHOTO-PROTECTEURS ADHÉSIFS ET LEURS UTILISATIONS
  申请人：SKINOSIVE

  公开号：WO2021123116A1

  公开（公告）日：2021-06-24

  The present invention relates to a compound represented by the following formula (I): A[B-(C)v]w, wherein A is a photoprotective moiety, B is a linker, C is a functional group, v is an integer from 1 to 2000, and w is an integer from 1 to 6. It also relates to a composition comprising the same and, more particularly, to a cosmetic or a sunscreen composition. It also relates to the use of such compounds in cosmetic and therapeutic applications. The invention also relates to the use of such compounds for reducing photodegradation and/or photoinstability of pharmaceuticals and cosmetics. The invention further relates to a material comprising a support and such a compound adhered to said support.

  本发明涉及一种由以下公式（I）表示的化合物：A[B-(C)v]w，其中A是光保护基团，B是连接基团，C是功能基团，v是从1到2000的整数，w是从1到6的整数。它还涉及包含该化合物的组合物，更具体地说，是化妆品或防晒霜组合物。还涉及在化妆品和治疗应用中使用这种化合物。该发明还涉及在药品和化妆品中减少光降解和/或光不稳定性的化合物的使用。该发明还涉及包含支撑物和该化合物粘附在该支撑物上的材料。
• 一种11-脱氢血栓烷素B2衍生物及其制备方法与11-脱氢血栓烷素B2检测试剂
  申请人：长沙博源医疗科技有限公司

  公开号：CN111825663B

  公开（公告）日：2023-08-18

  本发明公开了一种用于生物样本中11‑脱氢血栓烷素B2含量检测的11‑脱氢血栓烷素B2衍生物及其制备方法。使用该11‑脱氢血栓烷素B2衍生物获得了高免疫原性的11‑脱氢血栓烷素B2免疫原与抗11‑脱氢血栓烷素B2特异性抗体以及11‑脱氢血栓烷素B2‑多聚赖氨酸偶联物、抗11‑脱氢血栓烷素B2特异性抗体包被的胶乳颗粒等组份，并制备出了灵敏度高、特异性强、检测效果好的11‑脱氢血栓烷素B2免疫学检验试剂。本发明还提供了11‑脱氢血栓烷素B2免疫检验试剂的制备方法及相应的使用方法。本发明的11‑脱氢血栓烷素B2免疫检测方法克服了现有技术中11‑脱氢血栓烷素B2检测方法存在的操作复杂、自动化程度低等缺陷。
• PROTEIN AND PROTEIN CONJUGATE FOR DIABETES TREATMENT, AND APPLICATIONS THEREOF
  申请人：ADDA Biotech Inc.

  公开号：US20150183847A1

  公开（公告）日：2015-07-02

  The present invention relates to the field of biopharmaceutics, and in particular to a protein, a protein conjugate, a pharmaceutical composition and its use for treating diabetes. The fusion protein of the present invention is obtained by linking two polypeptides, wherein one polypeptide is an interleukin-1 receptor antagonistic protein or an analogue thereof, and another polypeptide is GLP-1 receptor binding polypeptide or an analogue thereof, or an insulin receptor binding polypeptide or an analogue thereof, or a GIP receptor binding polypeptide or an analogue thereof. The fusion proteins of the present invention and conjugates thereof have a significant efficacy in treating diabetes, and can be used in a lower dose, resulting in a marked reduction in side effects.

  本发明涉及生物制药领域，特别是一种蛋白质、蛋白质结合物、制药组合物及其治疗糖尿病的用途。本发明的融合蛋白质是通过连接两个多肽而获得的，其中一个多肽是白细胞介素-1受体拮抗蛋白或类似物，另一个多肽是GLP-1受体结合多肽或类似物，或胰岛素受体结合多肽或类似物，或GIP受体结合多肽或类似物。本发明的融合蛋白质及其结合物在治疗糖尿病方面具有显著的疗效，并且可以以较低剂量使用，从而显著减少副作用。
• 항체-약물 복합체 형성을 위한 이관능성 링커와 시스테인이 태그된 스파이태그/캐쳐를 이용한 고효율 접합 키트
  申请人：Biomax Co., Ltd. 주식회사 바이오맥스(120150289274) Corp. No ▼ 110111-5307651BRN ▼217-81-43469

  公开号：KR102235549B1

  公开（公告）日：2021-04-02

  ADC의 개발에 있어 항체와 약물의 안정적인 접합을 위한 연결자로서, 기존의 화학적 접합 방식과 번역 후 접합 방식의 단점을 개선한 보다 안정적이며 높은 접합 효율을 갖는 새로운 접합 키트가 개시된다. 본 발명은 항체-약물 복합체(Antibody-drug conjugates; ADC) 형성을 위한 항체 및 약물 간 접합 키트로서, 시스테인이 태그된(Cys-Tagged) 스파이태그(SpyTag) 올리고 펩타이드; 시스테인이 태그된(Cys-Tagged) 스파이캐쳐(SpyCatcher) 단백질; 및 상기 스파이태그 또는 상기 스파이캐쳐의 시스테인의 티올기에 접합되는 이관능성 링커(bifuctional cross-linker);를 포함하는 접합 키트를 제공한다.

  本发明提供了一种用于形成抗体-药物复合物（ADC）的抗体和药物之间的连接工具，以稳定地连接抗体和药物，改进了现有的化学连接方式和翻译后连接方式的缺点，具有更稳定和更高的连接效率的新连接工具。该发明包括带有半胱氨酸标记（Cys-Tagged）的SpyTag肽和带有半胱氨酸标记（Cys-Tagged）的SpyCatcher蛋白质以及连接到SpyTag或SpyCatcher的半胱氨酸硫醇官能团的双官能交联剂。
• PYRAZOLE-BASED CYANINE DYE
  申请人：Date Mutsuhiro

  公开号：US20090069546A1

  公开（公告）日：2009-03-12

  Problem Provided is a novel cyanine dye derivative with a pyrazole skeleton and an indole skeleton, having high sensitivity performance in a shorter wavelength region as compared with a conventional optical system, and showing high water solubility. Solution The invention provides (1) a compound represented by the following general formula [50] and a salt thereof: [wherein R 1 to R 6 each independently represent a substituted or unsubstituted alkyl group which may have an amide bond; R 7 to R 10 each independently represent alkyl group, alkenyl group, alkynyl group, aryl group, alkoxy group, aryloxy group, alkylthio group, arylthio group, alkylsulfonyl group, arylsulfonyl group, carbamoyl group, sulfamoyl group, ureido group or amino group, those groups being able to have substituents; a group represented by the general formula [2]: —COOR 12 [2] (wherein R 12 represents hydrogen atom, C 1 to C 10 alkyl group, alkali metal atom, organic ammonium ion, ammonium ion or anion); a group represented by the general formula [3]: —SO 3 R 13 [3] (wherein R 13 represents hydrogen atom, alkali metal atom, organic ammonium ion, ammonium ion or anion), halogen atom, aromatic heterocyclic thio group, hydrogen atom, hydroxyl group, cyano group, formyl group, thiol group or nitro group; R 11 represents hydrogen atom, or alkyl group, alkenyl group, alkynyl group or aryl group, those groups being able to have substituents; and n represents an integer of from 0 to 3, provided that any of R 1 and R 2 , R 4 and R 5 , R 1 and R 6 , and R 2 and R 4 may form a bivalent group with a group selected from —O— group, —S— group, —COO— group and groups represented by the general formulae [52] to [54]: (wherein R 50 represents hydrogen atom, alkyl group, alkenyl group or aryl group, those groups being able to have substituents), and substituted or unsubstituted alkylene group; and in the case where said bivalent group is formed, at least one of R 1 to R 11 , along with the bivalent group formed by any of R 1 and R 2 , R 4 and R 5 , R 1 and R 6 , and R 2 and R 4 , has the group represented by the general formula [2], the group represented by the general formula [3], amino group, hydroxyl group, thiol group or formyl group; and in the case where said bivalent group is not formed, at least one of R 1 to R 11 has the group represented by the general formula [2], the group represented by the general formula [3], amino group, hydroxyl group, thiol group or formyl group]; (2) a labeled compound obtained by subjecting the above compound to direct or indirect binding to a substance to be labeled, and (3) a method for labeling a substance to be labeled, comprising subjecting the above compound to direct or indirect binding to the substance to be labeled.

  问题提供了一种具有吡唑骨架和吲哚骨架的新型靛烯染料衍生物，与传统光学系统相比，在更短的波长区域具有高灵敏度性能，并且具有高水溶性。 解决方案提供了(1)以下一般式[50]及其盐所代表的化合物：[其中R1到R6各自独立地代表取代或未取代的烷基，该烷基可能具有酰胺键；R7到R10各自独立地代表烷基、烯基、炔基、芳基、烷氧基、芳氧基、烷硫基、芳硫基、烷磺酰基、芳基磺酰基、氨基甲酰基、磺酰胺基、脲基或氨基，这些基团能够具有取代基；由以下一般式[2]所代表的基团：—COOR12[2]（其中R12代表氢原子、C1到C10烷基、碱金属离子、有机铵离子、铵离子或阴离子）；由以下一般式[3]所代表的基团：—SO3R13[3]（其中R13代表氢原子、碱金属离子、有机铵离子、铵离子或阴离子）、卤素原子、芳基杂环硫基、氢原子、羟基、氰基、甲酰基、硫醇基或硝基；R11代表氢原子、或烷基、烯基、炔基或芳基，这些基团能够具有取代基；n代表从0到3的整数，前提是R1和R2、R4和R5、R1和R6以及R2和R4中的任何一个可以与选择自—O—基团、—S—基团、—COO—基团和由以下一般式[52]至[54]所代表的基团之一（其中R50代表氢原子、烷基、烯基或芳基，这些基团能够具有取代基）、取代或未取代的烷基烯基，形成双价基团；在形成双价基团的情况下，R1到R11中至少有一个与由R1和R2、R4和R5、R1和R6以及R2和R4中的任何一个形成的双价基团一起，具有由以下一般式[2]和[3]所代表的基团、氨基、羟基、硫醇基或甲酰基；在未形成双价基团的情况下，R1到R11中至少有一个具有由以下一般式[2]和[3]所代表的基团、氨基、羟基、硫醇基或甲酰基]；(2)通过将上述化合物直接或间接结合到待标记物质上而获得的标记化合物，以及(3)用于标记待标记物质的方法，包括将上述化合物直接或间接地结合到待标记物质上。