SUFUGOLIX
| 中文名称 | SUFUGOLIX |
|---|---|
| 中文同义词 | 舒夫戈利;化合物SUFUGOLIX |
| 英文名称 | SUFUGOLIX |
| 英文同义词 | SUFUGOLIX;TAK013;N-(4-(5-((benzyl(methyl)amino)methyl)-1-(2,6-difluorobenzyl)-1,2,3,4-tetrahydro-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl)phenyl)-N'-methoxyurea;TAK013;TAK 013;Sufugolix(TAK-013);SUFUGOLIX, >98%;tak-013, >98%;Urea, N-[4-[1-[(2,6-difluorophenyl)methyl]-1,2,3,4-tetrahydro-5-[[methyl(phenylmethyl)amino]methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]-N'-methoxy- |
| CAS号 | 308831-61-0 |
| 分子式 | C36H31F2N5O4S |
| 分子量 | 667.72 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 308831-61-0.mol |
| 结构式 |  |
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 |
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.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-100209 | SUFUGOLIX Sufugolix | 308831-61-0 | 5mg | 990元 |
| 2024/04/30 | HY-100209 | SUFUGOLIX Sufugolix | 308831-61-0 | 50mg | 6550元 |