Methyl-oxido-[[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxymethylimino]azanium | 14901-08-7

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: Methyl-oxido-[[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxymethylimino]azanium
• CAS: 14901-08-7
• 化学式: C8H16N2O7
• 分子量: 252.22
• InChiKey: YHLRMABUJXBLCK-JAJWTYFOSA-N

物化性质

• 熔点：
  154°C (rough estimate)
• 沸点：
  395.4°C (rough estimate)
• 比旋光度：
  D18 -44° (c = 0.62)
• 密度：
  1.4059 (rough estimate)
• 颜色/状态：
  COLORLESS, LONG NEEDLES
• 溶解度：
  READILY SOL IN WATER & DILUTE ETHANOL; INSOL IN BENZENE, CHLOROFORM, ETHYL ACETATE, ACETONE; SPARINGLY SOL IN ABSOLUTE ETHANOL
• 旋光度：
  SPECIFIC OPTICAL ROTATION: -44 DEG @ 18 °C/D (WATER, 0.62%); MAX ABSORPTION (0.4 MOLAR H2SO4): 217 NM
• 分解：
  When heated to decomposition it emits toxic fumes of /nitrogen oxides/.

计算性质

• 辛醇/水分配系数(LogP)：
  -2.6
• 重原子数：
  17
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  141
• 氢给体数：
  4
• 氢受体数：
  8

ADMET

代谢

CYCASIN在给予大鼠口服后，被肠道菌群中的β-葡萄糖苷酶分解，形成甲基氧化甲醇。

FOLLOWING ITS ORAL ADMIN TO RATS, CYCASIN IS SPLIT BY BETA-GLUCOSIDASE OF BACTERIAL FLORA TO FORM METHYLAZOXYMETHANOL.

来源:Hazardous Substances Data Bank (HSDB)

代谢

酶促水解/海枣苷/成甲基氧化甲醇在新生小鼠和大鼠的SC组织中也会发生，这些组织在出生后的早期阶段含有一种葡萄糖苷酶，这种酶在出生后的第14至25天消失。

ENZYMATIC HYDROLYSIS /OF CYCASIN/ TO METHYLAZOXYMETHANOL ALSO OCCURS IN SC TISSUES OF NEWBORN MICE & RATS, WHICH IN EARLY POSTNATAL PERIOD CONTAIN A GLUCOSIDASE THAT DISAPPEARS AFTER 14TH-25TH DAY OF LIFE.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 致癌性证据

没有关于人类的数据。有充分的证据表明对动物具有致癌性。总体评估：2B组：该物质可能对人类具有致癌性。

No data are available in humans. Sufficient evidence of carcinogenicity in animals. OVERALL EVALUATION: Group 2B: The agent is possibly carcinogenic to humans.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 致癌性证据

Cycasin: 作为合理预期的人类致癌物被除名。

Cycasin: delisted as reasonably anticipated to be a human carcinogen.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 致癌物分类

国际癌症研究机构致癌剂：环磷酰胺

IARC Carcinogenic Agent:Cycasin

来源:International Agency for Research on Cancer (IARC)

毒理性

• 致癌物分类

国际癌症研究机构（IARC）致癌物分类：2B组：可能对人类致癌

IARC Carcinogenic Classes:Group 2B: Possibly carcinogenic to humans

来源:International Agency for Research on Cancer (IARC)

毒理性

• 致癌物分类

国际癌症研究机构专著：第10卷：（1976年）一些天然存在的物质

IARC Monographs:Volume 10: (1976) Some Naturally Occurring Substances

来源:International Agency for Research on Cancer (IARC)

吸收、分配和排泄

CYCASIN和METHYLAZOXYMETHANOL /CYCASIN的代谢物/在大鼠和仓鼠中跨胎盘...

CYCASIN & METHYLAZOXYMETHANOL /METABOLITE OF CYCASIN/ CROSS PLACENTA IN RATS & HAMSTERS...

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

在口服给药后...对于常规和无菌大鼠，仅有24%...从常规大鼠的尿液和粪便中回收。在无菌大鼠中，回收率为100%。在大鼠通过胃管给予45-50毫克/只的剂量后，管理剂量的30-63%在尿液中回收。在大鼠进行腹腔注射后...95-100%...在24小时内从尿液中回收。

FOLLOWING ORAL ADMIN...TO CONVENTIONAL & GERM-FREE RATS ONLY 24%...RECOVERED IN URINE & FECES OF CONVENTIONAL RATS...100% IN...GERM-FREE RATS. IN RATS GIVEN 45-50 MG/ANIMAL BY STOMACH TUBE, 30-63% OF ADMIN DOSE WAS RECOVERED IN URINE. FOLLOWING IP INJECTION...IN RATS, 95-100%...RECOVERED FROM URINE WITHIN 24 HR.

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• 危险等级：
  6.1(b)
• 海关编码：
  2915900090
• 包装等级：
  III
• 危险类别：
  6.1(b)
• 危险品运输编号：
  UN 2811

文献信息

• [EN] BRUSH-ARM STAR POLYMERS, CONJUGATES AND PARTICLES, AND USES THEREOF<br/>[FR] POLYMÈRES EN ÉTOILE À BRAS EN BROSSE, CONJUGUÉS ET PARTICULES, ET LEURS UTILISATIONS
  申请人：MASSACHUSETTS INST TECHNOLOGY

  公开号：WO2018106738A1

  公开（公告）日：2018-06-14

  Described herein are macromonomers, conjugates comprising the macromonomers (also referred to alternatively as "BRUSH", or "BRUSH conjugates"), and brush arm star polymer particles comprising the conjugates (also referred to as "BASPs" or "BASP particles"), each further comprising an agent (e.g., one or more therapeutic agents, diagnostic agents, or targeting moieties), as well as starting materials (e.g., crosslinkers) and other components (e.g., degradation components) thereof, as well as pharmaceutical compositions and methods of making and using the same.

  本文描述了大单体、包含这些大单体的共轭物（也称为“刷子”或“刷子共轭物”），以及包含这些共轭物的刷子臂星形聚合物微粒（也称为“BASPs”或“BASP微粒），每种都进一步包含一种药剂（例如，一个或多个治疗药剂、诊断药剂或靶向基团），以及起始材料（例如，交联剂）和其他组分（例如，降解组分），以及制备和使用这些药物组合物的方法。
• Sterol glucoside toxins
  申请人：——

  公开号：US20040048810A1

  公开（公告）日：2004-03-11

  The invention relates to the identification of sterol glucoside toxins, and provides methods for detecting and detoxifying the compounds, as well as therapeutic methods for treating subjects exposed to such toxins. In alternative embodiments, the toxins may for example include beta-sitostrol-beta-D-glucoside (5-cholesten-24b-ethyl-3b-ol-D-glucoside) or cholesterol glucoside (5-cholesten-3b-ol-3b-D-glucoside).

  本发明涉及甾醇葡萄糖苷毒素的鉴定，并提供检测和解毒该化合物的方法，以及治疗暴露于此类毒素的受试者的治疗方法。在另一种实施方式中，毒素可以包括β-谷甾醇-β-D-葡萄糖苷（5-胆甾-24b-乙基-3b-醇-D-葡萄糖苷）或胆固醇葡萄糖苷（5-胆甾-3b-醇-3b-D-葡萄糖苷）等。
• Conditioning protocols and use of same for tissue regeneration
  申请人：Yeda Research and Development Co. Ltd.

  公开号：US10668109B2

  公开（公告）日：2020-06-02

  A method of conditioning a subject in need of transplantation of progenitor cells in suspension of a tissue of interest is disclosed. The method comprising: (a) administering to a subject a therapeutically effective amount of an agent capable of inducing damage to the tissue of interest, wherein the damage results in proliferation of resident stem cells in the tissue; and subsequently (b) subjecting the subject to an agent which ablates the resident stem cells in the tissue. A method of transplanting progenitor cells in suspension of a tissue of interest to a subject in need thereof is also disclosed.

  本发明公开了一种对需要移植悬浮于相关组织中的祖细胞的受试者进行调理的方法。该方法包括：(a) 向受试者施用治疗有效量的药剂，该药剂能够引起相关组织损伤，其中损伤导致组织中的常住干细胞增殖；随后(b) 使受试者接受消融组织中常住干细胞的药剂。此外，还公开了一种将相关组织悬浮液中的祖细胞移植给有需要的受试者的方法。
• Polyacetal polymers, conjugates, particles and uses thereof
  申请人：THE GENERAL HOSPITAL CORPORATION

  公开号：US11433136B2

  公开（公告）日：2022-09-06

  Provided herein are polymers, pH-sensitive polymers and/or linkers; conjugates comprising said polymers and/or linkers, optionally, coupled to one or more agents and/or targeting moieties; and particles (e.g., nanoparticles comprising the aforesaid polymers, linkers and/or conjugates), which can be used to enhance the delivery and/or efficacy of one or more agents in a subject.

  本文提供了聚合物、pH 值敏感聚合物和/或连接体；包含上述聚合物和/或连接体的共轭物（可选择与一种或多种制剂和/或靶向分子偶联）；以及颗粒（例如，包含上述聚合物、连接体和/或共轭物的纳米颗粒），可用于增强一种或多种制剂在受试者体内的递送和/或功效。
• Immunostimulatory nucleic acids and cancer medicament combination therapy for the treatment of cancer
  申请人：——

  公开号：US20020156033A1

  公开（公告）日：2002-10-24

  The invention involves administration of an immunostimulatory nucleic acid in combination with a cancer medicament for the treatment or prevention of cancer in subjects. The combination of drugs are administered in synergistic amounts or in various dosages or at various time schedules. The invention also relates to kits and compositions concerning the combination of drugs.

  本发明涉及将免疫刺激核酸与抗癌药物联合使用，用于治疗或预防受试者的癌症。药物组合以协同量或不同剂量或不同时间安排给药。本发明还涉及有关药物组合的试剂盒和组合物。