瑞索可托 | 76675-97-3

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 类固醇和类固醇衍生物
• 中文名称: 瑞索可托
• 英文名称: 4-pregnen-17, 21-diol-3, 20-dione
• 英文别名: 11-desoxycortisol；resocortol；(8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-10,13-dimethyl-17-propanoyl-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-3-one
• CAS: 76675-97-3
• 化学式: C₂₂H₃₂O₄
• 分子量: 360.494
• InChiKey: HERCGHIBUWWDIX-CWNVBEKCSA-N

物化性质

• 熔点：
  >218°C (dec.)
• 溶解度：
  DMSO（稍微加热）

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  26
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.82
• 拓扑面积：
  74.6
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  瑞索可托 在 Steroid-17,20-desmolase 作用下， 生成 4-雄烯-11β-醇-3,17-二酮 、 羟乙醛
  参考文献：
  名称：

  来自梭状芽孢杆菌ATCC 35704的desA和desB基因编码类固醇17，20-脱粘酶。

  摘要：

  梭菌梭状芽胞杆菌是一种能够去除皮质醇侧链并形成11β-氢-木二烯二酮的肠道微生物。之前，在皮质梭菌ATCC 35704中通过RNA-Seq鉴定了皮质醇诱导的操纵子（desABCD）。显示desC基因编码皮质醇20α-羟基类固醇脱氢酶（20α-HSDH）。desD编码一种注释为主要促进子家族成员的蛋白质，预计可充当皮质醇转运蛋白。desA和desB基因分别标注为N端和C端转酮酶。我们假设DesAB形成一个复合物，并具有类固醇17,20-脱摩尔酶活性。我们在pETDuet中从梭状芽胞杆菌ATCC 35704中克隆了desA和desB基因，以在大肠杆菌中过表达。纯化的重组DesAB被确定为142±5.4 kDa异源四聚体。我们开发了一种酶联连续分光光度法来定量类固醇17,20-脱糖酶。这是通过重组丝状真菌Cochliobolus lunatus的重组17β-HSDH将DesAB依赖性的11β-羟

  DOI：

  10.1194/jlr.m083949
• 作为产物：
  描述：

  在 过碘酸 作用下， 以 乙醇 为溶剂， 反应 0.03h， 以98%的产率得到瑞索可托
  参考文献：
  名称：

  高碘酸快速高效地从硫缩醛中再生甾体酮

  摘要：

  高碘酸在室温下在普通溶剂中通常能以高收率从其硫缩醛中平稳地再生出多种甾族酮。

  DOI：

  10.1039/c39800000886

文献信息

• Pharmaceutical preparation comprising an active dispersed on a matrix
  申请人：——

  公开号：US20040058896A1

  公开（公告）日：2004-03-25

  The present invention relates to the field of pharmaceutical technology and describes a novel advantageous preparation for an active ingredient. The novel preparation is suitable for producing a large number of pharmaceutical dosage forms. In the new preparation an active ingredient is present essentially uniformly dispersed in an excipient matrix composed of one or more excipients selected from the group of fatty alcohol, triglyceride, partial glyceride and fatty acid ester.

  本发明涉及制药技术领域，描述了一种新的有利的活性成分制备方法。这种新的制备方法适用于生产大量的药物剂型。在这种新的制备方法中，活性成分基本上均匀地分散在由脂肪醇、甘油三酯、部分甘油酯和脂肪酸酯等多种赋形剂中选择的一种或多种赋形剂组成的赋形剂基质中。
• Nitrate prodrugs able to release nitric oxide in a controlled and selective way and their use for prevention and treatment of inflammatory, ischemic and proliferative diseases
  申请人：Scaramuzzino, Giovanni

  公开号：EP1336602A1

  公开（公告）日：2003-08-20

  New pharmaceutical compounds of general formula (I): F-(X)q where q is an integer from 1 to 5, preferably 1; -F is chosen among drugs described in the text, -X is chosen among 4 groups -M, -T, -V and -Y as described in the text. The compounds of general formula (I) are nitrate prodrugs which can release nitric oxide in vivo in a controlled and selective way and without hypotensive side effects and for this reason they are useful for the preparation of medicines for prevention and treatment of inflammatory, ischemic, degenerative and proliferative diseases of musculoskeletal, tegumental, respiratory, gastrointestinal, genito-urinary and central nervous systems.

  通式（I）的新药物化合物：F-（X）q，其中q是1到5的整数，最好是1；-F是在文本中描述的药物中选择的，-X是在文本中描述的4个组-M，-T，-V和-Y中选择的。通式（I）的化合物是硝酸盐前药，可以在体内以受控和选择性的方式释放一氧化氮，而不会产生降压副作用，因此它们非常适用于制备用于预防和治疗肌肉骨骼，皮肤，呼吸，消化，泌尿和中枢神经系统的炎症，缺血，退行性和增生性疾病的药物。
• PHARMACEUTICAL PREPARATION COMPRISING AN ACTIVE DISPERSED ON A MATRIX
  申请人：ALTANA Pharma AG

  公开号：EP1341527A1

  公开（公告）日：2003-09-10
• COMPOSITIONS AND METHODS FOR MODULATING CIRCADIAN SYNCHRONIZATION
  申请人：Eichele Gregor

  公开号：US20120230978A1

  公开（公告）日：2012-09-13

  The present invention relates to a modulator of glucocorticoid biosynthesis, degradation and/or receptor activation for use in preventing or treating symptoms and/or diseases associated with jet lag. The compositions of the invention may be used as a lead compound for developing a drug for preventing or treating symptoms and/or diseases associated with jet lag. The invention relates to the discovery that administration of the modulator(s) to a subject results in a directional change of the time point of maximum amounts of glucocorticoids in the subject as compared to the time point of maximum amounts of glucocorticoids in a subject not treated with the modulator(s).
• METHODS OF CHEMOSELECTIVE DERIVATION OF MULTIPLE CLASSES OF METABOLITES
  申请人：Sello Jason K.

  公开号：US20130071940A1

  公开（公告）日：2013-03-21

  Chemoselective derivatization of biological amines, carboxylic acids, aldehydes or ketones are employed in methods to detect a plurality of components, or members of a component, such as metabolites, that vary in molecular structure. The methods of the invention can be employed in aqueous and nonaqueous conditions.