[(10S,13R,17R)-10,13-dimethyl-17-[(2R)-pentan-2-yl]-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl] 2-(methylamino)acetate

• 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
• 英文名称: [(10S,13R,17R)-10,13-dimethyl-17-[(2R)-pentan-2-yl]-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl] 2-(methylamino)acetate
• 化学式: C₂₇H₄₇NO₂
• 分子量: 417.7
• InChiKey: JZXOPGQHGCGABJ-JSJJMOICSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  8.2
• 重原子数：
  30
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.96
• 拓扑面积：
  38.3
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• Methods for treatment of bile acid-related disorders and prediction of clinical sensitivity to treatment of bile acid-related disorders
  申请人：NGM Biopharmaceuticals, Inc.

  公开号：US10434144B2

  公开（公告）日：2019-10-08

  Provided herein are methods of using 7a-hydroxy-4-cholsten-3-one (C4) in predicting the clinical sensitivity to treatment of bile acid-related and associated disorders with treatment peptides, such as variants of fibroblast growth factor 19 (FGF19) proteins and peptide sequences (and peptidomimetics) and fusions of FGF19 and/or fibroblast growth factor 21 (FGF21) proteins and peptide sequences (and peptidomimetics), and variants of fusions of FGF19 and/or FGF21 proteins and peptide sequences (and peptidomimetics).

  本文提供了使用7a-羟基-4-胆甾烯-3-酮（C4）来预测临床对治疗胆汁酸相关疾病和相关疾病的治疗肽的敏感性的方法、如成纤维细胞生长因子 19（FGF19）蛋白和多肽序列（和多肽模拟物）的变体、FGF19 和/或成纤维细胞生长因子 21（FGF21）蛋白和多肽序列（和多肽模拟物）的融合体，以及 FGF19 和/或 FGF21 蛋白和多肽序列（和多肽模拟物）融合体的变体。
• Methods and uses for modulating bile acid homeostasis and treatment of bile acid disorders and diseases
  申请人：NGM Biopharmaceuticals, Inc.

  公开号：US10456449B2

  公开（公告）日：2019-10-29

  Provided herein are methods of modulating bile acid homeostasis or treating a bile-acid related or associated disorder, comprising using variants and fusions of fibroblast growth factor 19 (FGF19), variants and fusions of fibroblast growth factor 21 (FGF21), fusions of FGF19 and/or FGF21, and variants or fusions of FGF19 and/or FGF21 proteins and peptide sequences (and peptidomimetics), in combination with agents effective in modulating bile acid homeostasis or treating a bile-acid related or associated disorder.

  本文提供了调节胆汁酸平衡或治疗胆汁酸相关或伴生疾病的方法，包括使用成纤维细胞生长因子19（FGF19）的变体和融合体、成纤维细胞生长因子21（FGF21）的变体和融合体、FGF19和/或FGF21的变体和融合体，以及FGF19和/或FGF21蛋白和多肽序列（和多肽模拟物）的变体或融合体，与有效调节胆汁酸稳态或治疗胆汁酸相关或伴发疾病的药物联合使用。
• Methods of using variants of FGF19 polypeptides for the treatment of pruritus
  申请人：NGM Biopharmaceuticals, Inc.

  公开号：US10744185B2

  公开（公告）日：2020-08-18

  Provided herein are variants of fibroblast growth factor 19 (FGF19) proteins and peptide sequences (and peptidomimetics) and fusions of FGF19 and/or fibroblast growth factor 21 (FGF21) proteins and peptide sequences (and peptidomimetics), and variants of fusions of FG-F19 and/or FGF21 proteins and peptide sequences (and peptidomimetics). In some embodiments, these variants and fusions modulate bile acid homeostasis, and are useful in treatment of bile acid related and associated disorders. In some embodiments, these variants and fusions have glucose lowering activity, and are useful in treatment of hyperglycemia and other disorders.

  本文提供的是成纤维细胞生长因子19（FGF19）蛋白和多肽序列（和多肽模拟物）的变体和FGF19和/或成纤维细胞生长因子21（FGF21）蛋白和多肽序列（和多肽模拟物）的融合物，以及FG-F19和/或FGF21蛋白和多肽序列（和多肽模拟物）融合物的变体。在某些实施方案中，这些变体和融合体可调节胆汁酸平衡，并可用于治疗胆汁酸相关疾病。在某些实施方案中，这些变体和融合体具有降糖活性，可用于治疗高血糖和其他疾病。
• METHODS FOR MODULATING BILE ACID HOMEOSTASIS AND TREATMENT OF BILE ACID DISORDERS AND DISEASES
  申请人：NGM Biopharmaceuticals, Inc.

  公开号：EP2938740A1

  公开（公告）日：2015-11-04
• CHIMERIC FGF19 PEPTIDES FOR USE IN TREATING BILE ACID DISORDERS
  申请人：NGM Biopharmaceuticals, Inc.

  公开号：EP2938740B1

  公开（公告）日：2022-04-20