60325-46-4
60325-46-4 结构式
基本信息
中文别名
硫前列酮舒普洛司通
素普罗斯顿
化合物 T23404
硫前列酮/SULPROSTONE
(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
英文别名
sch286SHB-286
Nalador
ZK-57671
CP-34089
CP-34086
SULPROSTONE
Sulprostone USP/EP/BP
Sulprostone >=95% (HPLC), oil
(1r-(1-alpha(z),2-beta(1e,3r*),3-alpha))--n-(methylsulfonyl)
所属类别
原料药：前列腺素类药物理化学性质
熔点79.25°C
密度1.1918 (rough estimate)
折射率1.5650 (estimate)
储存条件−20°C
储存条件-20°C
溶解度DMSO: >5 mg/mL
溶解度二甲基亚砜：>5 mg/mL
形态solid
颜色white to off-white
安全数据
警示词危险
危险性描述H315-H319-H335-H360
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 Germany3
WGK Germany3
RTECS号MJ8810000
毒性LD50 intraperitoneal in mouse: 18mg/kg
常见问题列表
用途
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。生物活性
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。靶点
|
EP3 Receptor
|
体外研究
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.
体内研究
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. |