硫前列酮
| 中文名称 | 硫前列酮 |
|---|---|
| 中文同义词 | 硫前列酮;素普罗斯顿;(Z)-7-[(1R,2R,3R)-3-羟基-2-((E,3R)-3-羟基-4-苯氧基-1-丁烯基)-5-氧代环戊基]-N-甲基磺酰基-5-庚烯酰胺;化合物 T23404;硫前列酮/SULPROSTONE;舒普洛司通 |
| 英文名称 | Sulprostone |
| 英文同义词 | (1r-(1-alpha(z),2-beta(1e,3r*),3-alpha))--n-(methylsulfonyl);16-phenoxy-17,18,19,20tetranorprostaglandine(sub2)methylsulfonylamide;16-phenoxy-omega-17,18,19,20-tetranorpge-2methylsulfonylamide;16-phenoxy-omega-17,18,19,20-tetranorprostaglandine2methylsulfonylamide;N-(METHYLSULFONYL)-9-OXO-11ALPHA,15R-DIHYDROXY-16-PHENOXY-17,18,19,20-TETRANOR-PROSTA-5Z,13E-DIEN-1-AMIDE;SHB-286;SULPROSTONE;ZK-57671 |
| CAS号 | 60325-46-4 |
| 分子式 | C23H31NO7S |
| 分子量 | 465.56 |
| EINECS号 | 262-173-0 |
| 相关类别 | 医药原料药;小分子 |
| Mol文件 | 60325-46-4.mol |
| 结构式 |  |
硫前列酮 性质
| 熔点 | 79.25°C |
|---|---|
| 密度 | 1.1918 (rough estimate) |
| 折射率 | 1.5650 (estimate) |
| 储存条件 | -20°C |
| 溶解度 | 二甲基亚砜：>5 mg/mL |
| 酸度系数(pKa) | 4.63±0.40(Predicted) |
| 形态 | 固体 |
| 颜色 | 白色至类白色 |
硫前列酮为前列腺素E2类似物，具有较强的子宫收缩作用，且作用较长，并具有较好的软化和扩张子宫颈管的作用。临床用于抗早孕、中期引产、扩宫颈及堕死胎等。Sulprostone (SHB 286) 是一种有效的，选择性的 EP3 受体激动剂。Sulprostone (SHB 286) 是一种前列腺素 E2 (PGE2) 类似物，具有抗溃疡和非甾体类抗流产作用。Sulprostone 有潜力用于终止妊娠和分娩时的出血。
|
EP3 Receptor
|
Sulprostone (SHB 286) has K
i
values of 21 nM and 0.6 nM for EP1 and EP3 in cultured Chinese hamster ovary cells.
Sulprostone (1, 1.5 or 2 mg/mL) does not significantly modify the viability and the purity of Dendritic cells (DCs). Sulprostone impairs spontaneous and directed DC migration independently from its concentration. Sulprostone reduces the expression of CCR7 and impairs migration of DCs.
Sulprostone (SHB 286; 0.5 mg/kg; IV) has a T
1/2
of 0.451 hours, a CL of 56 mL/min•kg, a V
ss
of 0.583 L/kg and an AUC of 149 ng•h/mL.
| Animal Model: | Male cynomolgus monkey |
| Dosage: | 0.5 mg/kg (Pharmacokinetic Analysis) |
| Administration: | IV |
| Result: | Had a T 1/2 of 0.451 hours, a CL of 56 mL/min•kg, a V ss of 0.583 L/kg and an AUC of 149 ng•h/mL. |
安全信息
| 危险品标志 | T |
|---|---|
| 危险类别码 | 60-36/37/38 |
| 安全说明 | 53-22-36/37-45 |
| WGK Germany | 3 |
| RTECS号 | MJ8810000 |
| 毒性 | LD50 intraperitoneal in mouse: 18mg/kg |