SUFUGOLIX
SUFUGOLIX 性质
| 密度 | 1.383±0.06 g/cm3(Predicted) |
|---|---|
| 储存条件 | Store at -20°C,unstable in solution, ready to use. |
| 溶解度 | DMF：5mg/mL； DMF:PBS (pH 7.2) (1:2)：0.3mg/mL；二甲基亚砜：3mg/mL |
| 形态 | 固体 |
| 酸度系数(pKa) | 13.20±0.70(Predicted) |
| 颜色 | 浅黄至黄色 |
SUFUGOLIX 用途与合成方法
IC50: 0.1 nM (human LHRH), 0.6 nM (monkey LHRH)
Sufugolix exhibits more than 3- and 2000-fold selectivity for the human receptor over the monkey and rat receptors, respectively. Sufugolix effectively antagonizes LHRH function on CHO cells expressing the human (IC 50 =0.1 nM) and monkey (IC 50 =0.6 nM) receptors. During the conformational analysis of sufugolix, using high-temperature molecular dynamics calculation, it is observed that the cis conformer of the methoxyurea is more populated than the trans conformer .
Oral administration of sufugolix causes almost complete suppression of the plasma LH levels in castrated male cynomolgus monkeys at a 30 mg/kg dose with sufficient duration of action (more than 24 h). The maximum plasma concentrations of sufugolix are 0.34 μM (reached 6 h after administration) and 0.18 μM (reached 4 h after administration) at 30 and 10 mg/kg doses, respectively.
SUFUGOLIX 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-11-08 | HY-100209 | 1 mg | 396 | ||
| 2024-11-08 | HY-100209 | SUFUGOLIX | 308831-61-0 | 5mg | 990 |
