Leu-leu甲酯氢溴酸 | 16689-14-8

• 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: Leu-leu甲酯氢溴酸
• 英文名称: H-Leu-Leu-OMe hydrobromide
• 英文别名: Leu-Leu-OMe hydrobromide；Leu-Leu-methyl ester hydrobromide；L-Leucine, L-leucyl-, methyl ester, monohydrobromide；methyl (2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-4-methylpentanoate;hydrobromide
• CAS: 16689-14-8
• 化学式: BrH*C₁₃H₂₆N₂O₃
• 分子量: 339.273
• InChiKey: QIPBCIHWFATZOF-ACMTZBLWSA-N

物化性质

• 溶解度：
  可溶于 DMSO（高达 35 mg/ml）或水（高达 40 mg/ml）

计算性质

• 辛醇/水分配系数(LogP)：
  1.64
• 重原子数：
  19
• 可旋转键数：
  8
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.85
• 拓扑面积：
  81.4
• 氢给体数：
  3
• 氢受体数：
  4

安全信息

• WGK Germany：
  3
• 海关编码：
  2924199090

制备方法与用途

生物活性

L-Leucyl-L-Leucine methyl ester (LLOMe) hydrobromide 是一种由人单核细胞或多形核白细胞产生的 L-亮氨酸甲酯的二肽缩合产物，能够选择性地消除具有细胞毒性潜能的淋巴细胞。此外，它还可以诱导溶酶体途径应激。

体外研究

在 MEFs 和 A549 细胞中，L-Leucyl-L-Leucine methyl ester (1 mM；0.5-2 小时) 可增强 LRRK2 介导的 Rab10 和 Rab12 的磷酸化。在 CD4- 淋巴细胞中，L-Leucyl-L-Leucine methyl ester (10-250 μM；15 分钟) 转化为一种 CCI3 COOH 不溶性产物。

反应信息

• 作为反应物：
  描述：

  Leu-leu甲酯氢溴酸 、 2-undec-10-enyl-tridec-12-enoic acid 在 1-羟基苯并三唑 、 三乙胺 、 N,N'-二异丙基碳二亚胺 作用下， 以 四氢呋喃 为溶剂， 反应 48.0h， 以71%的产率得到(S)-4-methyl-2-[4-methyl-2-(2-undec-10-enyltridec-12-enoylamino)pentanoylamino]pentanoic acid methyl ester
  参考文献：
  名称：

  ADMET Synthesis of Polyolefins Targeted for Biological Applications

  摘要：

  A series of "N-terminus" amino acid and peptide branched, chiral polyolefins, termed bioolefins, have been prepared using acyclic diene metathesis (ADMET) polycondensation chemistry, using a minimal amount of solvent and Grubbs' second generation catalyst. The carboxylic acid functional groups were protected with methyl, benzyl, and tert-butyl esters to enhance both the polymerizability of the monomers themselves and the solubility of the resulting polymers. A number of these polymers are semicrystalline, exhibiting melt transitions of up to 132 and 74 degreesC for the amino acid and dipeptide branched polymers, respectively. Adding a succinic acid spacer between the amino acid entity and the polymer backbone alters the melting behavior of the polymer, increasing the peak melting point by 27 degreesC when compared to a polymer having the same amino acid directly attached to the polymer backbone.

  DOI：

  10.1021/ma035289u

文献信息

• Preparation of fully human antibodies
  申请人：CCL Holdings Co., Ltd.

  公开号：EP1498426A1

  公开（公告）日：2005-01-19

  The present invention provides a method of preparing fully human antibodies that recognize a pre-determined antigen without relying on human donors that have already been exposed to the antigen. To this end, lymphocytes from naive human donors are immunized in vitro with the antigen of interest, and cells that produce antibodies against the antigen are identified. Since the lymphocytes are immunized in vitro rather than in vivo, it is possible to control which antigen, or which part of the antigen, would be recognized by the antibody. A preferred antigen is gp120 of HIV, particularly the co-receptor binding region of gp120.

  本发明提供了一种制备可识别预定抗原的全人抗体的方法，无需依赖已接触过抗原的人体供体。为此，用相关抗原体外免疫天真人类供体的淋巴细胞，并鉴定产生抗原抗体的细胞。由于淋巴细胞是在体外而不是体内免疫的，因此可以控制抗体识别哪种抗原或抗原的哪一部分。首选的抗原是艾滋病毒的 gp120，特别是 gp120 的共受体结合区。
• Monoclonal antibodies specific for different epitopes of human gp39 and methods for their use in diagnosis and therapy
  申请人：Bristol-Myers Squibb Company

  公开号：EP1728864A1

  公开（公告）日：2006-12-06

  The present invention provides monoclonal antibodies, antigen binding fragment and recombinant binding proteins specific for human gp39. These antibodies are specific for at least 12 different epitopes on gp39. Hybridomas secreting specific antibodies which bind to these epitopes are also provided. Further, the present invention discloses the amino acid sequence of immunoglobulin light and heavy chain variable regions which bind to epitopes of gp39 and provide sFv and humanized antibodies which bind gp39. Also, provided are pharmaceutical compositions comprising the monoclonal antibodies, antigen binding fragments and recombinant binding proteins which bind gp39 and methods for using these compositions in diagnosing disease states, inhibiting B cell activation and for treating immunological disorders, such as autoimmune diseases, allergic responses, organ rejection and graft-versus-host disease. Antibodies of the present invention can also be used to image cells which express gp39 on their surface, such as tumor cells (e.g., lymphoma) and to target therapeutic agents to target cells.

  本发明提供特异于人类 gp39 的单克隆抗体、抗原结合片段和重组结合蛋白。这些抗体对 gp39 上至少 12 个不同的表位具有特异性。本发明还提供了分泌与这些表位结合的特异性抗体的杂交瘤。此外，本发明还公开了与 gp39 表位结合的免疫球蛋白轻链和重链可变区的氨基酸序列，并提供了与 gp39 结合的 sFv 和人源化抗体。此外，还提供了包含结合 gp39 的单克隆抗体、抗原结合片段和重组结合蛋白的药物组合物，以及将这些组合物用于诊断疾病状态、抑制 B 细胞活化和治疗自身免疫性疾病、过敏反应、器官排斥和移植物抗宿主疾病等免疫学疾病的方法。本发明的抗体还可用于对表面表达 gp39 的细胞（如肿瘤细胞（如淋巴瘤））进行成像，并将治疗剂靶向靶细胞。
• Methods of generating high-production of antibodies from hybridomas created by in vitro immunization
  申请人：——

  公开号：US20040214288A1

  公开（公告）日：2004-10-28

  The invention provides methods for generating high titers of high-affinity antibodies from hybridoma cells produced by fusing myeloma cells with in vitro immunized donor cells. The hybridoma cells or mammalian expression cells with cloned antibody genes from the hybridomas producing the high-affinity antibodies may be mismatch repair defective due to defects of endogenous mismatch repair subunits of through expression of a dominant negative allele of a mismatch repair gene which allows the hybridoma cell to be hypermutable, may be rendered hypermutable by chemical means, or may be naturally mismatch repair deficient. High-affinity antibodies and high titer producer cells producing antibodies may be prepared by the methods of the invention.

  本发明提供了利用骨髓瘤细胞与体外免疫供体细胞融合产生的杂交瘤细胞产生高滴度高亲和力抗体的方法。产生高亲和力抗体的杂交瘤细胞或带有克隆抗体基因的哺乳动物表达细胞，可能由于内源性错配修复亚基的缺陷而存在错配修复缺陷，或由于表达了错配修复基因的显性阴性等位基因而使杂交瘤细胞具有高突变性，或通过化学方法使杂交瘤细胞具有高突变性，或可能天然存在错配修复缺陷。用本发明的方法可以制备高亲和力抗体和产生抗体的高滴度生产细胞。
• MONOCLONAL ANTIBODIES SPECIFIC FOR DIFFERENT EPITOPES OF HUMAN gp39 AND METHODS FOR THEIR USE IN DIAGNOSIS AND THERAPY
  申请人：Bristol-Myers Squibb Company

  公开号：EP0807175A2

  公开（公告）日：1997-11-19
• US5876950A
  申请人：——

  公开号：US5876950A

  公开（公告）日：1999-03-02