瑞卢戈利

• 常用名: 瑞卢戈利
• 英文名: Relugolix
• CAS号: 737789-87-6
• 分子量: 623.63
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₉H₂₇F₂N₇O₅S
• 熔点: N/A
• 闪点: N/A

瑞卢戈利用途

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.

瑞卢戈利名称

• 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

瑞卢戈利生物活性

• 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

瑞卢戈利物理化学性质

• 分子式: C₂₉H₂₇F₂N₇O₅S
• 分子量: 623.63
• PSA: 169.36000
• LogP: 3.96660
• InChIKey: AOMXMOCNKJTRQP-UHFFFAOYSA-N
• SMILES: CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nn2)c(=O)n3Cc2c(F)cccc2F)cc1
• 储存条件: 2-8℃

瑞卢戈利靶点实验

查看更多实验

实验名称：Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled h... 来源：ChEMBL 靶标：Gonadotropin-releasing hormone receptor External Id：CHEMBL4676203

实验名称：Cytotoxicity counterscreen for inhibitors of SARS-CoV-2 cell entry 来源：NCGC 靶标：N/A External Id：TRND-SARS-CoV-2-cytotox-48hr

实验名称：Primary qHTS to identify inhibitors of SARS-CoV-2 cell entry 来源：NCGC External Id：TRND-SARS-CoV-2-PP

实验名称：Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in C... 来源：ChEMBL 靶标：Gonadotropin-releasing hormone receptor External Id：CHEMBL1804376

实验名称：Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibit... 来源：ChEMBL 靶标：Gonadotropin-releasing hormone receptor External Id：CHEMBL1804378

实验名称：Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled h... 来源：ChEMBL 靶标：Gonadotropin-releasing hormone receptor External Id：CHEMBL4676202

实验名称：Inhibition of human CYP3A4 assessed as conversion of testosterone to 6beta-hydroxytes... 来源：ChEMBL 靶标：Cytochrome P450 3A4 External Id：CHEMBL1804377

实验名称：Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled h... 来源：ChEMBL 靶标：Gonadotropin-releasing hormone receptor External Id：CHEMBL4676201

实验名称：qHTS drug screen for cell cycle checkpoint inhibitors in PARPi-resistant BRCA-mutant ... 来源：NCGC External Id：FGL-PARP_PEO-CTG96h-MIPE5.0-p1

实验名称：Ratio IC50 for monkey GnRH receptor expressed in CHO cells as inhibition of GnRH-indu... 来源：ChEMBL 靶标：N/A External Id：CHEMBL1803295

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瑞卢戈利英文别名

• TAK-385
• Relugolix