3-hydroxy-estra-1,3,5(10)-trien-17-one

• 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: 3-hydroxy-estra-1,3,5(10)-trien-17-one
• 英文别名: (9S,13S,14S)-3-hydroxy-13-methyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-17-one
• 化学式: C₁₈H₂₂O₂
• 分子量: 270.371
• InChiKey: DNXHEGUUPJUMQT-QEWMCDCGSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  20
• 可旋转键数：
  0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.61
• 拓扑面积：
  37.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  3-hydroxy-estra-1,3,5(10)-trien-17-one 在 sodium cyanoborohydride 、 potassium carbonate 、 溶剂黄146 作用下， 以 四氢呋喃 、 N,N-二甲基甲酰胺 、 甲苯 、 丁酮 为溶剂， 反应 168.0h， 生成
  参考文献：
  名称：

  Non-peptide itam mimics as ZAP-70 antagonists

  摘要：

  Non-peptide bidentate ITAM mimics as ZAP-70 antagonists have been prepared by accommodating non-hydrolyzable phosphotyrosine analogues at each end of a non-peptide spacer with a maximal P-P distance of 39 Angstrom. The most potent antagonist 5 had an IC50=0.25 mu M against ZAP-70 with good cellular activity. Monodentates were ca. 10-fold weaker antagonists with improved cell permeability. (C) 1997 Elsevier Science Ltd.

  DOI：

  10.1016/s0960-894x(97)10102-0

文献信息

• FGF21 C-terminal peptide optimization
  申请人：INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION

  公开号：US11351268B2

  公开（公告）日：2022-06-07

  Disclosed herein are modified C-terminal fragments of FGF21 optimized for binding to Klotho β or antagonizing FGF21 activity. FGF21 peptides modified to comprise modifications to the C-terminal amino acid sequence are disclosed that have enhanced activity at the FGF21 receptor. Additionally, conjugates formed between the optimized FGF21 peptide fragments and insulin like peptides or nuclear hormone receptor ligands are provided.

  本文公开了经过修饰的 FGF21 C 端片段，这些片段经过优化，可与 Klotho β 结合或拮抗 FGF21 的活性。已公开的 FGF21 多肽包括对 C 端氨基酸序列的修饰，在 FGF21 受体上具有更强的活性。此外，还提供了优化的 FGF21 肽片段与胰岛素样肽或核激素受体配体之间形成的共轭物。
• System for providing birth control
  申请人：The Population Council, Inc.

  公开号：US11529308B2

  公开（公告）日：2022-12-20

  The present disclosure relates to a vaginal system that prevents pregnancy comprised of segesterone acetate and ethinyl estradiol and is configured for thirteen 28-day product-use cycles.

  本公开涉及一种阴道避孕系统，由醋酸雌二醇炔孕酮和炔雌醇组成，产品使用周期为 13 个 28 天。
• GLUCAGON SUPERFAMILY PEPTIDES EXHIBITING NUCLEAR HORMONE RECEPTOR ACTIVITY
  申请人：Indiana University Research and Technology Corporation

  公开号：EP2569000B1

  公开（公告）日：2017-09-27
• GLUCAGON SUPERFAMILY PEPTIDES EXHBITING G PROTEIN COUPLED RECEPTOR ACTIVITY
  申请人：Dimarchi Richard D.

  公开号：US20130116172A1

  公开（公告）日：2013-05-09

  Provided herein are glucagon superfamily peptides conjugated with GPCR ligands that are capable of acting at a G protein-coupled receptor. Also provided herein are pharmaceutical compositions and kits of the conjugates of the invention. Further provided herein are methods of treating a disease, e.g., a metabolic disorder, such as diabetes and obesity, comprising administering the conjugates of the invention.
• Glucagon Superfamily Peptides Exhibiting Nuclear Hormone Receptor Activity
  申请人：Indiana University Research and Technology Corporation

  公开号：US20150320871A1

  公开（公告）日：2015-11-12

  Provided herein are glucagon superfamily peptides conjugated with NHR ligands that are capable of acting at a nuclear hormone receptor. Also provided herein are pharmaceutical compositions and kits of the conjugates of the invention. Further provided herein are methods of treating a disease, e.g., a metabolic disorder, such as diabetes and obesity, comprising administering the conjugates of the invention.