ML-236B (compactin) | 125133-73-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 内酯类
• 英文名称: ML-236B (compactin)
• 英文别名: Mevastatin；4-hydroxy-6-{2-[2-methyl-8-(2-methyl-butyryloxy)-1,2,6,7,8,8a-hexahydro-naphthalen-1-yl]-ethyl}-tetrahydro-pyran-2-one；compactin；8-[2-(4-Hydroxy-6-oxotetrahydro-2h-pyran-2-yl)ethyl]-7-methyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl 2-methylbutanoate；[8-[2-(4-hydroxy-6-oxooxan-2-yl)ethyl]-7-methyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl] 2-methylbutanoate
• CAS: 125133-73-5
• 化学式: C₂₃H₃₄O₅
• 分子量: 390.52
• InChiKey: AJLFOPYRIVGYMJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  28
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.74
• 拓扑面积：
  72.8
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  ML-236B (compactin) 生成 7-[3,5-Dihydroxy-2-methyl-8-(2-methylbutanoyloxy)-1,2,3,5,6,7,8,8a-octahydronaphthalen-1-yl]-3,5-dihydroxyheptanoic acid
  参考文献：
  名称：

  TERAHARA, AKIRA;HAMANO, KIYOSHI;TSUJITA, YOSHIO;TANAKA, MINORU

  摘要：

  DOI：

文献信息

• [EN] ANTIOXIDANT, NEUROPROTECTIVE AND ANTINEOPLASTIC NANOPARTICLES COMPRISING A THERAPEUTIC AGENT ON AN AMPHIPHILIC SPACER OR AN AMPHIPHILIC POLYMER<br/>[FR] NANOPARTICULES ANTIOXYDANTES, NEUROPROTECTRICES ET ANTINÉOPLASIQUES COMPRENANT UN AGENT THÉRAPEUTIQUE SUR UN ESPACEUR AMPHIPHILE OU UN POLYMÈRE AMPHIPHILE
  申请人：CEDARS SINAI MEDICAL CENTER

  公开号：WO2013016696A1

  公开（公告）日：2013-01-31

  This invention relates to antioxidant, neuroprotective and antineoplastic nanoparticles comprising a therapeutic agent on an amphiphilic spacer or an amphiphilic polymer. Methods of synthesizing the antioxidant derivatives of camptothecin and antioxidant derivatives of camptothecin analogs, NSAIDs and statins, spontaneous emulsification or nanoprecipitation thereof to produce antioxidant, neuroprotective and anti-neoplastic nanoparticles comprising a therapeutic agent on an amphiphilic spacer or an amphiphilic polymer and their use in treating cancerous diseases are also provided. A further aspect of this invention is the use of these neuroprotective and anti-neoplastic nanoparticles for the preparation of delivery devices of other pharmaceuticals and/or drugs.

  本发明涉及抗氧化剂、神经保护剂和抗肿瘤纳米粒子，其包括具有治疗剂的两性亲脂间隔物或两性亲脂聚合物。还提供了合成伯氨替芬的抗氧化剂衍生物和伯氨替芬类似物、NSAIDs和他汀类药物的抗氧化剂衍生物的方法，以及通过自发乳化或纳米沉淀制备这些抗氧化、神经保护和抗肿瘤纳米粒子，其包括具有治疗剂的两性亲脂间隔物或两性亲脂聚合物，并且它们在治疗癌症疾病中的应用。本发明的另一个方面是利用这些神经保护和抗肿瘤纳米粒子制备其他药物和/或药物的输送装置。
• Model Animal for Pregnancy-induced Hypertension Syndrome, and Treatment Method Therefor
  申请人：Okabe Masaru

  公开号：US20150264901A1

  公开（公告）日：2015-09-24

  A lentiviral vector was used to produce non-human animals that express human sFLT1 specifically in the murine placenta, to provide model animals of diseases such as pregnancy-induced hypertension syndrome that are close to the clinical conditions, methods for producing the model animals, methods of screening for candidate compounds as therapeutic agents for diseases such as pregnancy-induced hypertension syndrome by using the model animals, and therapeutic agents for diseases such as pregnancy-induced hypertension syndrome. As a result, the model animals were found to exhibit symptoms that are very close to the clinical conditions in human, which are presentation of hypertension as well as placental insufficiency, intrauterine growth retardation, glomerulosclerosis, and proteinuria during pregnancy, and improvement of those symptoms postpartum. Furthermore, when pravastatin was administered to this model animal, it was found that diseases such as pregnancy-induced hypertension syndrome were improved by the activation of placenta-derived growth factor (PIGF) which antagonizes sFLT1.

  使用了一个lentiviral载体来产生非人类动物，这些动物在小鼠胎盘中特异性地表达人类sFLT1，以提供近似于临床情况的妊娠诱发高血压综合症等疾病的模型动物，以及制备该模型动物的方法，利用该模型动物筛选候选化合物作为治疗妊娠诱发高血压综合症等疾病的治疗剂的方法，以及用于治疗妊娠诱发高血压综合症等疾病的治疗剂。结果发现，模型动物表现出与人类临床情况非常接近的症状，包括妊娠期高血压、胎盘功能不全、胎儿宫内生长迟缓、肾小球硬化和蛋白尿，以及产后这些症状的改善。此外，当普伐他汀被用于该模型动物时，发现通过激活胎盘源性生长因子（PIGF）来对抗sFLT1可以改善妊娠诱发高血压综合症等疾病。
• MODEL ANIMAL FOR PREGNANCY-INDUCED HYPERTENSION SYNDROME, AND TREATMENT METHOD THEREFOR
  申请人：Okabe, Masaru

  公开号：EP2543729A1

  公开（公告）日：2013-01-09

  A lentiviral vector was used to produce non-human animals that express human sFLT1 specifically in the murine placenta, to provide model animals of diseases such as pregnancy-induced hypertension syndrome that are close to the clinical conditions, methods for producing the model animals, methods of screening for candidate compounds as therapeutic agents for diseases such as pregnancy-induced hypertension syndrome by using the model animals, and therapeutic agents for diseases such as pregnancy-induced hypertension syndrome. As a result, the model animals were found to exhibit symptoms that are very close to the clinical conditions in human, which are presentation of hypertension as well as placental insufficiency, intrauterine growth retardation, glomerulosclerosis, and proteinuria during pregnancy, and improvement of those symptoms postpartum. Furthermore, when pravastatin was administered to this model animal, it was found that diseases such as pregnancy-induced hypertension syndrome were improved by the activation of placenta-derived growth factor (PIGF) which antagonizes sFLT1.

  利用慢病毒载体生产在小鼠胎盘中特异表达人sFLT1的非人类动物，提供与临床症状接近的妊娠诱发高血压综合征等疾病的模型动物、生产模型动物的方法、利用模型动物筛选治疗妊娠诱发高血压综合征等疾病的候选化合物的方法，以及治疗妊娠诱发高血压综合征等疾病的药物。结果发现，模型动物表现出的症状与人类的临床症状非常接近，即在妊娠期间出现高血压以及胎盘功能不全、宫内发育迟缓、肾小球硬化和蛋白尿，并在产后改善这些症状。此外，在给该模型动物服用普伐他汀后，发现妊娠诱发高血压综合征等疾病可通过激活可拮抗 sFLT1 的胎盘衍生生长因子（PIGF）而得到改善。
• Murakawa, Shigeo; Nakamura, Takeshi; Komagata, Daisuke, Agricultural and Biological Chemistry, 1987, vol. 51, # 7, p. 1879 - 1884
  作者：Murakawa, Shigeo、Nakamura, Takeshi、Komagata, Daisuke、Sunagawa, Emi、Endo, Akira

  DOI：——

  日期：——
• ENDO, AKIRA;YAMASHITA, HARUYUKI
  作者：ENDO, AKIRA、YAMASHITA, HARUYUKI

  DOI：——

  日期：——

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