2-脱氧-L-葡糖 | 25029-33-8

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 脂肪酰基
• 中文名称: 2-脱氧-L-葡糖
• 英文名称: 2-Deoxy-L-arabino-hexose
• 英文别名: 2-Desoxy-L-glucose；2-Desoxy-L-arabino-hexose；2-Deoxy-L-glucose；2-deoxy-D-galactose；L-arabino-2-deoxy-hexose；2-deoxygalactose；(3S,4R,5S)-3,4,5,6-tetrahydroxyhexanal
• CAS: 25029-33-8
• 化学式: C₆H₁₂O₅
• 分子量: 164.158
• InChiKey: VRYALKFFQXWPIH-HCWXCVPCSA-N

物化性质

• 沸点：
  456.7±45.0 °C(Predicted)
• 密度：
  1.414±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -2.9
• 重原子数：
  11
• 可旋转键数：
  5
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  98
• 氢给体数：
  4
• 氢受体数：
  5

ADMET

代谢

2-脱氧-D-葡萄糖在小鼠睾丸和肝脏中转化为6-磷酸，这是在连续7天每天以50毫克/千克体重的剂量腹腔注射后的结果。

2-DEOXY-D-GLUCOSE WAS CONVERTED TO THE 6-PHOSPHATE IN MOUSE TESTIS AND LIVER AFTER IP INJECTION OF 50 MG/KG BODY WT DAILY FOR 7 DAYS.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

大量腹腔注射2-脱氧葡萄糖在大鼠中引起了视网膜电图的变化，表现为α和β波的降低。这种效应被D-葡萄糖所拮抗。

2-DEOXYGLUCOSE INJECTED INTRAPERITONEALLY IN RATS IN LARGE DOSES CAUSED CHANGES IN THE ELECTRORETINOGRAM CONSISTING OF A DECR IN BOTH ALPHA- AND BETA-WAVES. THE EFFECT WAS ANTAGONIZED BY D-GLUCOSE.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

同时给予超过其最大肾小管转运能力的葡萄糖剂量，抑制了2-脱氧葡萄糖的肾小管重吸收。因此，肾小管重吸收的过程可能与葡萄糖相同。

SIMULTANEOUS ADMIN OF GLUCOSE @ DOSE EXCEEDING ITS MAX TUBULAR TRANSPORT CAPACITY INHIBITED TUBULAR REABSORPTION OF 2-DEOXYGLUCOSE. THUS, THE PROCESS OF TUBULAR REABSORPTION IS PROBABLY THE SAME AS THAT FOR GLUCOSE.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

在乏情期绵羊中，2-脱氧葡萄糖输注抑制了由雌二醇诱导的促黄体生成素（LH）的释放，但并未抑制由促黄体生成素释放激素（LH-RH）诱导的LH释放。

IN ANESTROUS SHEEP, 2-DEOXYGLUCOSE INFUSION INHIBITED LH RELEASE INDUCED BY ESTRADIOL BUT NOT BY LH-RH.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

2-脱氧-D-葡萄糖抑制了X射线在小鼠艾利希腹水癌细胞中引起的潜在致命损伤的修复。

2-DEOXY-D-GLUCOSE INHIBITED REPAIR OF POTENTIALLY LETHAL DAMAGE INDUCED BY X-RAYS IN MOUSE EHRLICH ASCITES TUMOR CELLS.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 非人类毒性摘录

在大剂量注射2-脱氧葡萄糖到大鼠的腹膜腔内，引起了视网膜电图的变化，表现为α波和β波的降低。

2-DEOXYGLUCOSE INJECTED INTRAPERITONEALLY IN RATS IN LARGE DOSES CAUSED CHANGES IN THE ELECTRORETINOGRAM CONSISTING OF A DECR IN BOTH ALPHA- AND BETA-WAVES.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

当使用常规清除和停止流动技术研究狗和老鼠的肾脏对2-脱氧葡萄糖的排泄时，发现肾小管对其重吸收的比例平均为68-89%，重吸收部位位于近端小管。

WHEN THE RENAL EXCRETION OF 2-DEOXYGLUCOSE WAS STUDIED IN DOGS AND RATS BY CONVENTIONAL CLEARANCE AND STOP-FLOW TECHNIQUES, IT WAS REABSORBED BY THE RENAL TUBULES AT AN AVG OF 68-89% OF THE FILTERED LOADS AND THE REABSORPTION SITE WAS IN THE PROXIMAL TUBULES.

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• 海关编码：
  2912491000

文献信息

• [EN] PROSTATE-SPECIFIC MEMBRANE ANTIGEN ANTIBODY DRUG CONJUGATES<br/>[FR] CONJUGUÉS ANTICORPS-MÉDICAMENT D'ANTIGÈNE MEMBRANAIRE SPÉCIFIQUE À LA PROSTATE
  申请人：AMBRX INC

  公开号：WO2013185117A1

  公开（公告）日：2013-12-12

  This invention relates to prostate-specific membrane antigen (PSMA) antibodies and antibody drug conjugates comprising at least one non-naturally-encoded amino acid. Disclosed herein are αPSMA antibodies with one or more non-naturally encoded amino acids and further disclosed are antibody drug conjugates wherein the αPSMA antibodies of the invention are conjugated to one or more toxins. Also disclosed herein are non-natural amino acid dolastatin analogs that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such dolastatin analogs. Typically, the modified dolastatin analogs include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid antibody drug conjugates, dolastatin analogs, and modified non-natural amino acid dolastatin analogs, including therapeutic, diagnostic, and other biotechnology uses.

  本发明涉及前列腺特异性膜抗原（PSMA）抗体及包含至少一个非天然编码氨基酸的抗体药物偶联物。公开了具有一个或多个非天然编码氨基酸的αPSMA抗体，以及进一步公开了抗体药物偶联物，其中本发明的αPSMA抗体与一个或多个毒素偶联。还公开了非天然氨基酸多拉司汀类似物，这些类似物在翻译后进一步修饰，以及实现这些修饰的方法和纯化这些多拉司汀类似物的方法。通常，修饰的多拉司汀类似物包括至少一个肟、羰基、二羰基和/或羟基胺基团。进一步公开了使用此类非天然氨基酸抗体药物偶联物、多拉司汀类似物和修饰的非天然氨基酸多拉司汀类似物的方法，包括治疗、诊断和其他生物技术用途。
• Modified Human Apolipoprotein A-1 and Their Uses
  申请人：Knudsen Nick

  公开号：US20110178029A1

  公开（公告）日：2011-07-21

  Modified human apolipoprotein A-I polypeptides and uses thereof are provided.

  提供了改良的人类载脂蛋白A-I多肽及其用途。
• MODIFIED RELAXIN POLYPEPTIDES AND THEIR USES
  申请人：KRAYNOV Vadim

  公开号：US20120046229A1

  公开（公告）日：2012-02-23

  Modified relaxin polypeptides and their uses thereof are provided

  修改后的弛缓素多肽及其用途
• Modified Leptin Polypeptides and Their Uses
  申请人：Kraynov Vadim

  公开号：US20120149636A1

  公开（公告）日：2012-06-14

  Modified human leptin polypeptides and uses thereof are provided.

  提供了改良的人类瘦素多肽及其用途。
• [EN] RAPAMYCIN CARBOHYDRATE DERIVATIVES<br/>[FR] DERIVES DE RAPAMYCINE CARBOHYDRATE
  申请人：ISOTECHNIKA INTERNAT INC

  公开号：WO2004101583A1

  公开（公告）日：2004-11-25

  This invention provides modified rapamycins that have specific monosaccharide(s), oligosaccharide(s), pseudosugar(s) or derivatives thereof attached through a linker to create rapamycin carbohydrate derivatives having enhanced pharmacokinetic and/or pharmacodynamic profiles. For example, administration of the rapamycin carbohydrate derivative results in altered pharmacokinetic profiles and reduced toxicities. Thus, the present invention provides compounds with characteristics that are distinct from other drugs in its class such as rapamycin.

  这项发明提供了经过改良的雷帕霉素，其具有通过连接剂连接的特定单糖，寡糖，伪糖或其衍生物，从而创造出具有增强药代动力学和/或药效动力学特性的雷帕霉素糖衍生物。例如，给予雷帕霉素糖衍生物的治疗导致了改变的药代动力学特性和降低的毒性。因此，本发明提供了具有与其他同类药物（如雷帕霉素）不同特性的化合物。