SUFUGOLIX
|
|
|
- CAS号:
- 308831-61-0
- 英文名:
- SUFUGOLIX
- 英文别名:
- TAK013;SUFUGOLIX;tak-013, >98%;TAK013;TAK 013;SUFUGOLIX, >98%;Sufugolix(TAK-013);Sufugolix, 10 mM in DMSO;TAK 013,Inhibitor,Sufugolix,inhibit,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;TAK-013 1-(4-(5-((benzyl(methyl)amino)methyl)-1-(2,6-difluorobenzyl)-2,4-dioxo-3-phenyl-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-3-methoxyurea
- 中文名:
- SUFUGOLIX
- 中文别名:
- 舒夫戈利;化合物SUFUGOLIX;化合物SUFUGOLIX,10 MM DMSO 溶液
- CBNumber:
- CB12451333
- 分子式:
- C36H31F2N5O4S
- 分子量:
- 667.72
- MOL File:
- 308831-61-0.mol
|
|
|
SUFUGOLIX化学性质
-
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; DMSO: 3mg/mL
-
|
-
形态:
-
A solid
-
|
-
酸度系数(pKa):
-
13.20±0.70(Predicted)
-
|
-
颜色:
-
Light yellow to yellow
-
|
SUFUGOLIX性质、用途与生产工艺
Sufugolix (TAK-013)高效有口服活性的黄体激素释放激素 (LHRH) 受体拮抗剂，IC50值为0.1 nM。
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
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2025/02/08 | HY-100209 | Sufugolix | 308831-61-0 | 1 mg | 396元 |
| 2025/02/08 | HY-100209 | SUFUGOLIX
Sufugolix | 308831-61-0 | 5mg | 990元 |
308831-61-0, SUFUGOLIX 相关搜索:
- 抑制剂
- 化合物SUFUGOLIX,10 MM DMSO 溶液
- 化合物SUFUGOLIX
- 舒夫戈利
- 308831-61-0
- Sufugolix, 10 mM in DMSO
- TAK 013,Inhibitor,Sufugolix,inhibit,TAK013
- TAK-013 1-(4-(5-((benzyl(methyl)amino)methyl)-1-(2,6-difluorobenzyl)-2,4-dioxo-3-phenyl-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-3-methoxyurea
- 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-
- tak-013, >98%
- SUFUGOLIX, >98%
- Sufugolix(TAK-013)
- TAK013;TAK 013
- 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
- SUFUGOLIX