737789-87-6

• 常用中文名：瑞卢戈利
• 常用英文名：Relugolix
• CAS号：737789-87-6
• 分子式：C₂₉H₂₇F₂N₇O₅S
• 分子量：623.63
• 相关类别： 信号通路 G 蛋白偶联受体/G 蛋白 GNRH受体
• 发布时间：2018-06-03 08:00:00
• 更新时间：2026-07-02 02:07:48
• Relugolix是一个新颖的，非肽的能够口服的GnRH拮抗剂，IC50值是0.33 nM.

名称

• 中文名: 瑞卢戈利
• 英文名: 1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea
• 中文别名: 1-(4-(1-(2,6-二氟苄基)-5-((二甲基氨基)甲基)-3-(6-甲氧基哒嗪-3-基)-2,4-二氧代-1,2,3,4-四氢噻吩并[2,3-D]嘧啶-6-基)苯基)-3-甲氧基脲; 瑞卢戈利对照品; Relugolix瑞卢戈利; 1-(4-(1-(2,6-二氟苄基)-5-((二甲胺基)甲基)-3-(6-甲氧基哒嗪-3-基)-2,4-二氧代-1,2,3,4-四氢噻吩并[2,3-D]嘧啶-6-基)苯基)-3-甲氧基脲; 瑞卢戈利 (TAK-385); RVT-601|||瑞卢戈利|||TAK-385; 瑞卢戈利粗品; 瑞卢戈利相关杂质; 1-(4-(1-(2,6-二氟苄基)-5-((二甲基氨基)甲基)-3-(6-甲氧基哒嗪-3-基)-2,4-二氧-1,2,3,4-四氢噻吩并[2,3-D]嘧啶-6-基)苯基)-3-甲氧基脲,瑞卢戈利; N- [4- [1 - [(2,6-二氟苯基)甲基]-5 - [(二甲基氨基)甲基] -1,2,3,4-四氢-3-(6-甲氧基-3-哒嗪基) - 2,4-二氧噻吩并[2,3-D]嘧啶-6-基]苯基] -N'-甲氧基脲; 雷卢戈利克斯; 瑞卢戈利及中间体、杂质; N-[4-[1-[(2,6-二氟苯基)甲基]-5-[(二甲基氨基)甲基]-1,2,3,4-四氢-3-(6-甲氧基-3-吡嗪基)-2,4-二氧噻吩并[2,3-D]嘧啶-6-基]苯基]-N'-甲氧基脲; RELUGOLIX瑞卢戈利 TAK-385; 瑞卢戈利Relugolix; RELUGOLIX游离态; 瑞卢戈利/精确称量; 1-(4-(1-(2,6-二氟苄基)-5-((二甲基氨基)甲基)-3-(6-甲氧基哒嗪-3-基)-2,4-二氧-1,2,3,4-四氢噻吩并[2,3-D]嘧啶-6-基)苯基)-3-甲氧基脲; 瑞卢戈利,10 MM DMSO 溶液
• 英文别名: 2H6]-RVT-601; ethyl 5-(4-aminophenyl)-2-((2,6-difluorobenzyl)(ethoxycbonyl)amino)-4-((dimethylamino)methyl)thiophene-3-cboxylate; Rui Lugoli; 10G,G,G; Cefime hydrochloride anhydrous; TAK-385;TAK 385;TAK; RVT-601|||TAK-385; Urea, N-[4-[1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-1,2,3,4-tetrahydro-3-(6-methoxy-3-pyridazinyl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-N'-methoxy; TAK-385; RVT-601; Relugolix Impurity 17; TKA-385 Relugolix; ruiugoli; A60%,B; Relugolix (1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea); N-[4-[1-[(2,6-Difluorophenyl)methyl]-5-[(dimethylamino)methyl]-1,2,3,4-tetrahydro-3-(6-methoxy-3-pyridazinyl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-N'-methoxy urea; Relugoli; N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenylcbamoyl)-N-methoxybutyramide; Altropane; 1-[4-[1-[(2,6-difluorophenyl)methyl]-5-(dimethylaminomethyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-6-thieno[4,5-e]pyrimidinyl]phenyl]-3-methoxyurea; TAK-385,Relugolix; Relugolix(NEC-1); Rui Lu Geli; 1-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydro thieno[2,3-d]pyrimidin-6-yl)phenyl)-3-methoxy urea, Relugolix; Relugolix TAK-385; Relugolix, 10 mM in DMSO

物化性质

• 分子式: C₂₉H₂₇F₂N₇O₅S
• 分子量: 623.63
• PSA: 169.36000
• LogP: 3.96660
• 储存条件: 2-8℃

生物活性

• 描述: Relugolix是一个新颖的,非肽的能够口服的GnRH拮抗剂,IC50值是0.33 nM.
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> GNRH受体
  研究领域 >> 癌症
• 参考文献:

  [1]. MacLean DB et al. Medical Castration Using the Investigational Oral GnRH Antagonist TAK-385 (Relugolix): Phase 1 Study in Healthy Males. J Clin Endocrinol Metab. 2015 Dec;100(12):4579-87.

  [2]. Nakata D et al. Suppression of the hypothalamic-pituitary-gonadal axis by TAK-385 (relugolix), a novel, investigational, orally active, small molecule gonadotropin-releasing hormone (GnRH) antagonist: studies in human GnRH receptor knock-in mice. Eur J Ph