3-(4-Bromo-2-ethoxyphenyl)acrylic acid | 1094474-73-3

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 肉桂酸及其衍生物
• 英文名称: 3-(4-Bromo-2-ethoxyphenyl)acrylic acid
• 英文别名: (E)-3-(4-bromo-2-ethoxyphenyl)prop-2-enoic acid
• CAS: 1094474-73-3
• 化学式: C₁₁H₁₁BrO₃
• 分子量: 271.11
• InChiKey: ZZCUVOHRNAJVOM-GQCTYLIASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  15
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  46.5
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• Human G protein-coupled receptors and modulators thereof for the treatment of metabolic-related disorders
  申请人：Arena Pharmaceuticals, Inc.

  公开号：US20040142377A1

  公开（公告）日：2004-07-22

  The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In preferred embodiments, the GPCR is human. In other preferred embodiments, the GPCR is coupled to Gi and lowers the level of intracellular cAMP. In other preferred embodiments, the GPCR is expressed endogenously by adipocytes. In further preferred embodiments, the GPCR inhibits intracellular lipolysis. In other further preferred embodiments, the GPCR is a nicotinic acid receptor. The present invention also relates to methods of using a modulator of said GPCR. Preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, stroke, insulin resistance, and type 2 diabetes.

  本发明涉及鉴定候选化合物是否为 G 蛋白偶联受体（GPCR）调节剂的方法。在优选的实施方案中，GPCR 是人类的。在其他优选的实施方案中，GPCR 与 Gi 相耦合，降低细胞内 cAMP 的水平。在其他优选的实施方案中，GPCR 由脂肪细胞内源表达。在更多优选的实施方案中，GPCR 可抑制细胞内脂肪分解。在其他更优选的实施方案中，GPCR 是烟酸受体。本发明还涉及使用所述 GPCR 的调节剂的方法。优选的调节剂是激动剂。本发明的激动剂可用作预防或治疗代谢相关疾病的治疗剂，包括血脂异常、动脉粥样硬化、冠心病、中风、胰岛素抵抗和 2 型糖尿病。
• Human G Protein-Coupled Receptors and Modulators Thereof for the Treatment of Metabolic-Related Disorders
  申请人：Unett David J.

  公开号：US20110177612A1

  公开（公告）日：2011-07-21

  The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In preferred embodiments, the GPCR is human. In other preferred embodiments, the GPCR is coupled to Gi and lowers the level of intracellular cAMP. In other preferred embodiments, the GPCR is expressed endogenously by adipocytes. In further preferred embodiments, the GPCR inhibits intracellular lipolysis. In other further preferred embodiments, the GPCR is a nicotinic acid receptor. The present invention also relates to methods of using a modulator of said GPCR. Preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, stroke, insulin resistance, and type 2 diabetes.
• US6902902B2
  申请人：——

  公开号：US6902902B2

  公开（公告）日：2005-06-07
• US7829298B2
  申请人：——

  公开号：US7829298B2

  公开（公告）日：2010-11-09