DY142 | 1106977-71-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: DY142
• 英文别名: (3-{3-[(2,2-diphenylethyl)-(3-trifluoromethylbenzyl)amino]propoxy}phenyl)acetic acid；(3-{3-[(2,2-Diphenyl-ethyl)-(3-trifluoromethyl-benzyl)-amino]-propoxy}-phenyl)-acetic acid；2-[3-[3-[2,2-diphenylethyl-[[3-(trifluoromethyl)phenyl]methyl]amino]propoxy]phenyl]acetic acid
• CAS: 1106977-71-2
• 化学式: C₃₃H₃₂F₃NO₃
• 分子量: 547.617
• InChiKey: WCRVRZSYNQUNJL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.3
• 重原子数：
  40
• 可旋转键数：
  13
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  49.8
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  (3-{3-[(2,2-Diphenyl-ethyl)-(3-trifluoromethyl-benzyl)-amino]-propoxy}-phenyl)-acetic acid methyl ester 在 sodium hydroxide 、 水 、 盐酸 作用下， 以 甲醇 、 水 、 乙酸乙酯 为溶剂， 以87%的产率得到DY142
  参考文献：
  名称：

  SYNTHETIC LIGANDS SELECTIVE FOR LXRbeta OVER LXRalpha, IDENTIFICATION AND METHODS OF USE THEREOF

  摘要：

  LXR核受体激动剂先前已被证明可以增加胆固醇外流，提高血浆HDL胆固醇，刺激胆固醇排泄，并减少动脉粥样硬化病变。然而，这些激动剂也与不良的副作用高三酸甘油脂血症有关。这种高三酸甘油脂血症似乎是由LXRα亚型介导的，而不是LXRβ，这表明LXRβ选择性激动剂是调节人类脂质代谢的理想候选药物。本申请提供了新颖的LXRβ选择性配体，优先调节LXRβ而非LXRα。这些配体可用于治疗与LXR相关的多种疾病，例如脂质代谢紊乱、动脉粥样硬化、阿尔茨海默病和炎症。

  公开号：

  US20090030082A1

文献信息

• Synthetic ligands selective for LXRβ over LXRα, identification and methods of use thereof
  申请人：Forman Barry

  公开号：US08993628B2

  公开（公告）日：2015-03-31

  LXR nuclear receptor agonists have been previously shown to increase cholesterol efflux, raise plasma HDL cholesterol, stimulate cholesterol excretion, and reduce atherosclerotic lesions. However, these agonists have also been associated with the unwanted side effect of hypertriglyeridemia. This hypertriglyeridemia appears to be mediated by the LXRα subtype rather than LXRβ, which suggests that LXRβ-selective agonists are attractive candidates for modulation of human lipid metabolism. The present application provides novel LXRβ-selective ligands that preferably modulate LXRβ over LXRα. These ligands may be used to treat a variety of diseases associated with LXR, such as for example lipid metabolism disorders, atherosclerosis, Alzheimer disease, and inflammation.

  LXR核受体激动剂以前已被证明可以增加胆固醇外流，提高血浆高密度脂蛋白胆固醇，刺激胆固醇排泄和减少动脉粥样硬化斑块。然而，这些激动剂也与不良的高三酰甘油血症副作用相关。这种高三酰甘油血症似乎是由LXRα亚型介导的，而不是LXRβ，这表明LXRβ选择性激动剂是调节人类脂质代谢的有吸引力的候选药物。本申请提供了新的LXRβ选择性配体，它们更倾向于调节LXRβ而不是LXRα。这些配体可以用于治疗与LXR相关的各种疾病，例如脂质代谢紊乱、动脉粥样硬化、阿尔茨海默病和炎症。
• METHOD OF INHIBITING TREM-1
  申请人：THE SCRIPPS RESEARCH INSTITUTE

  公开号：US20220117965A1

  公开（公告）日：2022-04-21

  Disclosed herein are methods and uses of the polypharmacological modulator SR1903 and related compounds for inhibiting triggering receptor expressed on myeloid cells-1 (TREM-1) and treating diseases and conditions that are related to or mediated by TREM-1, such as inflammatory diseases, autoimmune diseases, metabolic disorders, and castration resistant prostate cancer (CRPC).
• US8993628B2
  申请人：——

  公开号：US8993628B2

  公开（公告）日：2015-03-31
• SYNTHETIC LIGANDS SELECTIVE FOR LXRbeta OVER LXRalpha, IDENTIFICATION AND METHODS OF USE THEREOF
  申请人：Forman Barry

  公开号：US20090030082A1

  公开（公告）日：2009-01-29

  LXR nuclear receptor agonists have been previously shown to increase cholesterol efflux, raise plasma HDL cholesterol, stimulate cholesterol excretion, and reduce atherosclerotic lesions. However, these agonists have also been associated with the unwanted side effect of hypertriglyeridemia. This hypertriglyeridemia appears to be mediated by the LXRα subtype rather than LXRβ, which suggests that LXRβ-selective agonists are attractive candidates for modulation of human lipid metabolism. The present application provides novel LXRβ-selective ligands that preferably modulate LXRβ over LXRα. These ligands may be used to treat a variety of diseases associated with LXR, such as for example lipid metabolism disorders, atherosclerosis, Alzheimer disease, and inflammation.

  LXR核受体激动剂先前已被证明可以增加胆固醇外流，提高血浆HDL胆固醇，刺激胆固醇排泄，并减少动脉粥样硬化病变。然而，这些激动剂也与不良的副作用高三酸甘油脂血症有关。这种高三酸甘油脂血症似乎是由LXRα亚型介导的，而不是LXRβ，这表明LXRβ选择性激动剂是调节人类脂质代谢的理想候选药物。本申请提供了新颖的LXRβ选择性配体，优先调节LXRβ而非LXRα。这些配体可用于治疗与LXR相关的多种疾病，例如脂质代谢紊乱、动脉粥样硬化、阿尔茨海默病和炎症。