6-Lactoyltetrahydropterin | 33405-80-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 蝶啶及其衍生物
• 英文名称: 6-Lactoyltetrahydropterin
• 英文别名: 2-amino-6-(2-hydroxypropanoyl)-5,6,7,8-tetrahydro-3H-pteridin-4-one
• CAS: 33405-80-0
• 化学式: C₉H₁₃N₅O₃
• 分子量: 239.23
• InChiKey: HKCYZTKHPLJZDR-UHFFFAOYSA-N

物化性质

• 沸点：
  478.3±55.0 °C(Predicted)
• 密度：
  1.88±0.1 g/cm3(Predicted)
• 物理描述：
  Solid

计算性质

• 辛醇/水分配系数(LogP)：
  -1.6
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  129
• 氢给体数：
  5
• 氢受体数：
  5

文献信息

• Clinical applications of tetrahydrobiopterin, lipoic acid and their salts and methods of preparing tetrahydrobiopterin bis-lipoate
  申请人：Richardson T. Kenneth

  公开号：US20060194808A1

  公开（公告）日：2006-08-31

  Dosage forms and methods of use are disclosed for: a) the simultaneous administration of tetrahydrobiopterin (BH4) or a derivative, homolog or precursor thereof and lipoic acid (LA), or dihydrolipoic acid (DHLA), or a derivative, homolog or salt thereof or, b) the administration of a conjugate consisting of tetrahydrobiopterin bis-lipoate (TBL). The invention is useful for the amelioration of diabetes mellitus types 1 and 2 (including impaired glucose tolerance, pre-diabetes, insulin resistance, metabolic syndrome X and as an adjunct to oral antidiabetic agents and/or insulin), diabetic and non-diabetic microvascular diseases (including nephropathy, neuropathy and retinopathy), diabetic and non-diabetic macrovascular diseases (including heart attack, stroke, peripheral vascular disease and ischemia-reperfusion injury), hypertension, vasoconstriction, obesity, dyslipedemia, and neurodegenerative disorders (including Parkinson's disease, mild cognitive impairment, senile dementia, Alzheimer's disease, hearing loss and chronic glaucomas). A novel method for the preparation of TBL is also disclosed.

  本发明揭示了以下的剂型和使用方法：a) 同时给药四氢生物蝶啶（BH4）或其衍生物、同系物或前体以及硫辛酸（LA）或二氢硫辛酸（DHLA），或其衍生物、同系物或盐；b) 给药由四氢生物蝶啶双硫辛酸酯（TBL）组成的结合物。本发明可用于改善糖尿病类型1和2（包括糖耐量受损、糖尿病前期、胰岛素抵抗、代谢综合征X以及作为口服抗糖尿病药物和/或胰岛素的辅助剂），糖尿病和非糖尿病微血管疾病（包括肾病、神经病变和视网膜病变），糖尿病和非糖尿病大血管疾病（包括心脏病发作、中风、外周血管疾病和缺血再灌注损伤），高血压、血管收缩、肥胖、血脂异常和神经退行性疾病（包括帕金森病、轻度认知障碍、老年痴呆症、听力丧失和慢性青光眼）。本发明还揭示了一种制备TBL的新方法。
• Probe compound for detecting and isolating enzymes and means and methods using the same
  申请人：Helmholtz-Zentrum für Infektionsforschung GmbH

  公开号：EP2230312A1

  公开（公告）日：2010-09-22

  The present invention relates to a probe compound that can comprise any substrate or metabolite of an enzymatic reaction in addition to an indicator component, such as, for example, a fluorescence dye, or the like. Moreover, the present invention relates to means for detecting enzymes in form of an array, which comprises any number of probe compounds of the invention which each comprise a different metabolite of interconnected metabolites representing the central pathways in all forms of life. Moreover, the present invention relates to a method for detecting enzymes involving the application of cell extracts or the like to the array of the invention which leads to reproducible enzymatic reactions with the substrates. These specific enzymatic reactions trigger the indicator (e.g. a fluorescence signal) and bind the enzymes to the respective cognate substrates. Moreover, the invention relates to means for isolating enzymes in form of nanoparticles coated with the probe compound of the invention. The immobilisation of the cognate substrates or metabolites on the surface of nanoparticles by means of the probe compounds allows capturing and isolating the respective enzyme, e.g. for subsequent sequencing.

  本发明涉及一种探针化合物，它可以包括酶反应的任何底物或代谢物，此外还包括指示成分，例如荧光染料或类似物。此外，本发明还涉及以阵列形式检测酶的方法，该阵列由任意数量的本发明探针化合物组成，每种探针化合物由代表所有生命形式中中心途径的相互关联的代谢物中的不同代谢物组成。此外，本发明还涉及一种检测酶的方法，该方法涉及将细胞提取物或类似物应用于本发明的阵列，从而导致与底物发生可重复的酶反应。这些特定的酶反应会触发指示剂（如荧光信号），并将酶与各自的同源底物结合。此外，本发明还涉及以涂覆有本发明探针化合物的纳米颗粒形式分离酶的方法。通过探针化合物将同源底物或代谢物固定在纳米颗粒表面，可以捕获和分离相应的酶，例如用于后续测序。
• METHOD FOR PRODUCING SEPIAPTERIN AND TETRAHYDROLACTOYLPTERIN
  申请人：Shiratori Pharmaceutical Co., Ltd.

  公开号：EP2848619B1

  公开（公告）日：2018-07-11
• Clinical Applications of Tetrahydrobiopterin, Lipoic Acid and Their Salts and Methods of Preparing Tetrahydrobiopterin Bis-Lipoate
  申请人：Richardson Kenneth T.

  公开号：US20090068264A1

  公开（公告）日：2009-03-12

  Dosage forms and methods of use are disclosed for: a) the simultaneous administration of tetrahydrobiopterin (BH4) or a derivative, homolog or precursor thereof and lipoic acid (LA), or dihydrolipoic acid (DHLA), or a derivative, homolog or salt thereof or, b) the administration of a conjugate consisting of tetrahydrobiopterin bis-lipoate (TBL). The invention is useful for the amelioration of diabetes mellitus types 1 and 2 (including impaired glucose tolerance, pre-diabetes, insulin resistance, metabolic syndrome X and as an adjunct to oral antidiabetic agents and/or insulin), diabetic and non-diabetic microvascular diseases (including nephropathy, neuropathy and retinopathy), diabetic and non-diabetic macrovascular diseases (including heart attack, stroke, peripheral vascular disease and ischemia-reperfusion injury), hypertension, vasoconstriction, obesity, dyslipedemia, and neurodegenerative disorders (including Parkinson's disease, mild cognitive impairment, senile dementia, Alzheimer's disease, hearing loss and chronic glaucomas). A novel method for the preparation of TBL is also disclosed.
• Method for Producing Biopterins Using Tetrahydrobiopterin Biosynthesis Enzyme
  申请人：Shimizu Ichiro

  公开号：US20090104668A1

  公开（公告）日：2009-04-23

  Biopterins are useful compounds utilized in pharmaceutical agents or functional foods. The presence of sepiapterin reductase (SPR) involved in the biosynthesis of biopterins has not been confirmed so far in microorganisms except for a few microorganisms such as blue-green algae. For efficiently producing biopterins using microorganisms, it has been demanded to obtain and use SPR genes derived from microorganisms. The present inventors have found that when Saccharomyces cerevisiae or Escherichia coli is transformed with a YIR035C gene from Saccharomyces cerevisiae or a yueD gene from Bacillus subtilis , the transformed microorganism secretes biopterins into a culture solution. Based on this finding, the present invention provides a polypeptide, DNA encoding the polypeptide, a recombinant vector comprising the DNA, and a transformant obtained by transformation with the vector, which are useful in biopterin production using microorganisms. Moreover, the present invention provides a method for efficiently producing biopterins using the transformant.