货号 | 2519/1 |
别名 | 7-[(2,6-Difluorophenyl)methyl]-4,7- |
供应商 | Tocris |
生物活性 | Potent, orally active and non-peptide gonadotropin-releasing hormone (GnRH, LHRH) receptor antagonist (IC50 values are 0.2, 4.0 and 60 nM for human, monkey and rat GnRH receptors respectively). Inhibits LH release in vitro(IC50 = 100 nM) and reduces plasma LH concentration in castrated male cynomolgus monkeys. |
运输条件 | Blue Ice |
存放说明 | 4℃ |
纯度 | >98 % |
计算分子量 | 657.77 |
分子式 | C37H37F2N3O4S |
可溶性/溶解性 | Soluble to 50 mM in DMSO |
CAS号 | 192887-28-8 |
参考文献 | Imadaet al (2006) Design, synthesis, and structure-activity relationships of thieno[2,3-b]pyridin-4-one derivatives as a novel class of potent, orally active, non-peptide luteinizing hormone-releasing hormone receptor antagonists. J.Med.Chem. 49 3809. PMID: 16789738. Sasakiet al (2003) Discovery of a thieno[2,3-d]pyrimidine-2,4-dione bearing a p-methoxyureidophenyl moiety at the 6-position: a highly potent and orally bioavailable non-peptide antagonist for the human luteinizing hormone-releasing hormone receptor. J.Med.Chem. 46 113. PMID: 12502365. Choet al (1998) Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor. J.Med.Chem. 41 4190. PMID: 9784092. |