Sufugolix (TAK-013) is a potent and orally available luteinizing hormone-releasing hormone LHRH receptor.

LHRH:0.1 nM.

Sufugolix在针对人类受体与猴子及大鼠受体的选择性上分别展现出超过3倍与2000倍的差异。在表达人类(IC50=0.1 nM)及猴子(IC50=0.6 nM)受体的CHO细胞上，Sufugolix有效地拮抗LHRH功能。在进行Sufugolix构象分析时，通过高温分子动力学计算观察到，甲氧基脲的顺式构象比反式构象具有更高的占比[1]。

通过口服sufugolix，在剂量为30 mg/kg时，几乎可以完全抑制去势雄性猕猴的血浆LH水平，并且作用持续时间充分（超过24小时）。Sufugolix具有明显的亲脂性，从而增加了膜的渗透性并相应改善了在猕猴体内的口服吸收。Sufugolix的最大血浆浓度分别在剂量为30 mg/kg和10 mg/kg时达到0.34 μM（服药后6小时）和0.18 μM（服药后4小时）[1]。

The receptor-expressing CHO cells are seeded into 24-well plates at a density of 4×104 cells/well and cultured for 1 day. The cells are then incubated with [5,6,8,9,11,12,14,15-3H]arachidonic acid (11 kBq/well) for 1 day and ished with DMEM supplemented with 20 mM HEPES and 0.2% BSA. The cells are then preincubated with the compounds (Sufugolix) at 37 °C for 60 min and the reaction is started by addition of LHRH (1 nM). After incubation at37 °C for 40 min, radioactivity in the medium is measured with a liquid scintillation counter[1].