(S)-FTY-phosphonate | 1142015-10-8

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: (S)-FTY-phosphonate
• 英文别名: (S)-FTY720 phosphonate；(3S)-3-amino-3-(hydroxymethyl)-5-(4'-octylphenyl)pentylphosphonic acid；(S)-FTY-720Phosphonate；[(3S)-3-amino-3-(hydroxymethyl)-5-(4-octylphenyl)pentyl]phosphonic acid
• CAS: 1142015-10-8
• 化学式: C₂₀H₃₆NO₄P
• 分子量: 385.484
• InChiKey: XDSPSYJWGHPIAZ-FQEVSTJZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  26
• 可旋转键数：
  14
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.7
• 拓扑面积：
  104
• 氢给体数：
  4
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  (S)-FTY720 Vinylphosphonate 在 10% Pd(OH)2 on carbon 、 氢气 作用下， 以 甲醇 为溶剂， 以91%的产率得到(S)-FTY-phosphonate
  参考文献：
  名称：

  免疫抑制剂 FTY720 的手性乙烯基膦酸酯和膦酸酯类似物

  摘要：

  描述了 FTY720 的手性等排膦酸酯类似物的第一个对映选择性合成。其中一个类似物 FTY720-( E )-乙烯基膦酸酯 ( S )- 5，而不是它的R对映异构体，在肠上皮细胞中引起有效的抗凋亡作用，表明它通过受体的对映选择性激活发挥作用。( S ) -5未能激活 1-磷酸鞘氨醇 1 型 (S1P 1 ) 受体。

  DOI：

  10.1021/jo900023u

文献信息

• Method Of Treating Acute Lung Injury Using Sphingosine 1 Phosphate Analogs Or Sphingosine 1 Phosphate Receptor Agonists
  申请人：Garcia Joe G.N.

  公开号：US20130079309A1

  公开（公告）日：2013-03-28

  The invention provides methods for treating or reducing the risk of developing acute lung injury manifested by increased vascular permeability. Also provided are pharmaceutical compositions comprising an FTY720 analog or derivative and/or SEW 2871 for use in the disclosed methods. The invention also provides methods for treating or reducing the risk of developing acute lung injury resulting from dysregulation of ceramide/sphingolipid pathway, more specifically, acute lung injury resulting from radiation.

  本发明提供了治疗或减少因增加血管通透性而表现为急性肺损伤的方法。还提供了包含FTY720类似物或衍生物和/或SEW 2871的药物组合物，用于所述方法。本发明还提供了治疗或减少因鞘氨醇/鞘脂代谢通路失调而导致的急性肺损伤的方法，更具体地说，是由放射线引起的急性肺损伤。
• Stabilization of alcohol intoxication-induced cardiovascular instability
  申请人：Breslin Jerome William

  公开号：US10111841B2

  公开（公告）日：2018-10-30

  The present invention concerns use of an agent that increases sphingosine-1-phosphate (S1P) receptor activity, such as S1P, or an S1P receptor agonist, for treatment of alcohol-intoxicated subjects will help stabilize blood pressure and improve resuscitation efforts in alcohol-intoxicated subjects, including alcohol-intoxicated trauma patients. Another aspect concerns a kit for stabilization of alcohol-intoxicated subjects, comprising an agent that increases S1P receptor activity.

  本发明涉及一种增加鞘氨醇-1-磷酸（S1P）受体活性的药剂，如 S1P 或 S1P 受体激动剂，用于治疗酒精中毒者，将有助于稳定血压和改善酒精中毒者（包括酒精中毒的创伤患者）的复苏工作。另一个方面涉及一种用于稳定酒精中毒受试者的试剂盒，其中包含一种能提高 S1P 受体活性的制剂。
• STABILIZATION OF ALCOHOL INTOXICATION-INDUCED CARDIOVASCULAR INSTABILITY
  申请人：BRESLIN JEROME WILLIAM

  公开号：US20170020826A1

  公开（公告）日：2017-01-26

  The present invention concerns use of an agent that increases sphingosine-1-phosphate (S1P) receptor activity, such as S1P, or an S1P receptor agonist, for treatment of alcohol-intoxicated subjects will help stabilize blood pressure and improve resuscitation efforts in alcohol-intoxicated subjects, including alcohol-intoxicated trauma patients. Another aspect concerns a kit for stabilization of alcohol-intoxicated subjects, comprising an agent that increases S1P receptor activity.