海参素A | 38-26-6

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 异戊烯醇脂质
• 中文名称: 海参素A
• 英文名称: holothurin A
• 英文别名: sodium;[(3R,4R,5R,6S)-5-[(2S,3R,4R,5S,6R)-5-[(2S,3R,4S,5R,6R)-4-[(2S,3R,4S,5R,6R)-3,5-dihydroxy-6-(hydroxymethyl)-4-methoxyoxan-2-yl]oxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-3,4-dihydroxy-6-methyloxan-2-yl]oxy-6-[[(1S,2S,5R,6S,9S,10S,13S,16S,18R)-6-[(2S)-5,5-dimethyloxolan-2-yl]-5,10-dihydroxy-2,6,13,17,17-pentamethyl-8-oxo-7-oxapentacyclo[10.8.0.02,9.05,9.013,18]icos-11-en-16-yl]oxy]-4-hydroxyoxan-3-yl] sulfate
• CAS: 38-26-6
• 化学式: C₅₄H₈₅O₂₇S*Na
• 分子量: 1221.31
• InChiKey: KXDQPKMJSMCBEY-VOFJYVFSSA-M

物化性质

• 熔点：
  239-240 °C

计算性质

• 辛醇/水分配系数(LogP)：
  -5.6
• 重原子数：
  83
• 可旋转键数：
  13
• 环数：
  10.0
• sp3杂化的碳原子比例：
  0.94
• 拓扑面积：
  416
• 氢给体数：
  11
• 氢受体数：
  27

文献信息

• Human serum albumin linkers and conjugates thereof
  申请人：Merrimack Pharmaceuticals, Inc.

  公开号：EP2860260A1

  公开（公告）日：2015-04-15

  The present invention relates to a human serum albumin (HSA) linker and binding, diagnostic, and therapeutic agents conjugated thereto. Also disclosed are methods and kits for the diagnostic and therapeutic application of an HSA linker conjugate.

  本发明涉及一种人血清白蛋白（HSA）连接体及其结合剂、诊断剂和治疗剂。还公开了 HSA 连接体共轭物的诊断和治疗应用方法及试剂盒。
• Conjugates that are configured for targeted delivery of therapeutic compounds to senescent cells
  申请人：Unity Biotechnology, Inc.

  公开号：US10745445B2

  公开（公告）日：2020-08-18

  Disclosed are agents (e.g., peptides, polypeptides, proteins, small molecules, antibodies, and antibody fragments that target senescent cells) and methods of their use for imaging senescent cells in vivo and for treating or preventing cancer, age-related disease, tobacco-related disease, or other diseases and disorders related to or caused by cellular senescence in a mammal. The methods include administering one or more of the agents of the invention to a mammal, e.g., a human. The agents, which specifically bind to senescent cells, can be labeled with a radioactive label or a therapeutic label, e.g., a cytotoxic agent.

  本发明公开了靶向衰老细胞的制剂（例如肽、多肽、蛋白质、小分子、抗体和抗体片段）及其使用方法，用于体内衰老细胞成像和治疗或预防癌症、老年相关疾病、烟草相关疾病或与哺乳动物细胞衰老有关或由细胞衰老引起的其他疾病和紊乱。这些方法包括向哺乳动物（如人类）施用一种或多种本发明制剂。这些能与衰老细胞特异性结合的制剂可以用放射性标签或治疗性标签（如细胞毒性制剂）标记。
• Compositions and methods for the treatment and prevention of neurological disorders
  申请人：Yumanity Therapeutics, Inc.

  公开号：US11241417B2

  公开（公告）日：2022-02-08

  The invention provides compositions and methods for treating neurological disorders, such as amyotrophic lateral sclerosis, frontotemporal degeneration, and Alzheimer's disease, among others. Using the compositions and methods described herein, a patient having a neurological disorder, such as a neurological disorder associated with TAR-DNA binding protein (TDP)-43 aggregation, may be administered an inhibitor of cytochrome P450 (CYP450) isoform 51A1 (CYP51A1), also referred to herein as lanosterol 14-alpha demethylase, so as to treat an underlying etiology of the disorder and/or to alleviate one or more symptoms of the disease. The inhibitor of CYP51A1 may be a small molecule, anti-CYP51A1 antibody or antigen-binding fragment thereof, or a compound, such as an interfering RNA molecule, that attenuates CYP51A1 expression. Patients that may be treated using the compositions and methods described herein include those that express a mutant TDP-43 isoform containing a mutation associated with TDP-43-promoted aggregation and toxicity.

  本发明提供了治疗神经系统疾病的组合物和方法，如肌萎缩侧索硬化症、额颞变性和阿尔茨海默病等。使用本文所述的组合物和方法，可以给患有神经系统疾病（如与TAR-DNA结合蛋白（TDP）-43聚集相关的神经系统疾病）的患者施用细胞色素P450（CYP450）同工酶51A1（CYP51A1）的抑制剂，CYP51A1在本文中也称为羊毛甾醇14-α去甲基化酶，从而治疗该疾病的潜在病因和/或减轻该疾病的一种或多种症状。CYP51A1的抑制剂可以是小分子、抗CYP51A1抗体或其抗原结合片段，或者是减弱CYP51A1表达的化合物，如干扰RNA分子。可使用本文所述组合物和方法治疗的患者包括那些表达突变型 TDP-43 同工酶的患者，这种突变与 TDP-43 促进的聚集和毒性有关。
• HUMAN SERUM ALBUMIN LINKERS AND CONJUGATES THEREOF
  申请人：Merrimack Pharmaceuticals, Inc.

  公开号：EP2288715A2

  公开（公告）日：2011-03-02
• METHODS AND COMPOSITIONS FOR PROSTATE CANCER IMMUNOTHERAPY
  申请人：Beth Israel Deaconess Medical Center

  公开号：EP2300040A2

  公开（公告）日：2011-03-30