1-methyl-3-[(Z)-(4-oxo-3-prop-2-enyl-1,3-thiazolidin-2-ylidene)amino]thiourea

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 1-methyl-3-[(Z)-(4-oxo-3-prop-2-enyl-1,3-thiazolidin-2-ylidene)amino]thiourea
• 化学式: C₈H₁₂N₄OS₂
• 分子量: 244.3
• InChiKey: DDYJDIHOSRTMSE-FLIBITNWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  114
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• Thiourea derivatives as activators of RORα and pharmaceutical composition containing same
  申请人：Lee Mi Ock

  公开号：US10407388B2

  公开（公告）日：2019-09-10

  Provided is a compound activating RORα gene, particularly a JC1 compound containing CGP52608 thiazolidinedione as a lead substance, and a pharmaceutically acceptable salt thereof. The compound is a lipid accumulation inhibitor and applicable to the treatment of metabolic diseases or inflammatory diseases.

  本研究提供了一种激活 RORα 基因的化合物，特别是一种以 CGP52608 噻唑烷二酮为先导物质的 JC1 化合物及其药学上可接受的盐。该化合物是一种脂质蓄积抑制剂，适用于治疗代谢性疾病或炎症性疾病。
• 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。
• 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
• Anti-PSMA Antibodies Conjugated to Nuclear Receptor Ligand Polypeptides
  申请人：Ambrx, Inc.

  公开号：US20150152187A1

  公开（公告）日：2015-06-04

  This invention relates to anti-prostate-specific membrane antigen antibodies (αPSMA) and αPSMA antibody—nuclear receptor ligand (NRL) conjugates comprising at least one non-naturally-encoded amino acid.
• 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.