4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate
| 中文名称 | 4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate |
|---|---|
| 中文同义词 | 化合物 PATAMOSTAT |
| 英文名称 | 4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate |
| 英文同义词 | 4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate;4-Guanidinobenzoic acid 4-[[2-(2,5-dioxopyrrolidin-1-yl)ethyl]thio]phenyl ester;Patomostat;Benzoic acid, 4-[(aminoiminomethyl)amino]-, 4-[[2-(2,5-dioxo-1-pyrrolidinyl)ethyl]thio]phenyl ester |
| CAS号 | 114568-26-2 |
| 分子式 | C20H20N4O4S |
| 分子量 | 412.46 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 114568-26-2.mol |
| 结构式 |  |
4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate 性质
| 熔点 | 201.6 °C |
|---|---|
| 沸点 | 653.2±65.0 °C(Predicted) |
| 密度 | 1.41±0.1 g/cm3(Predicted) |
| 储存条件 | 4°C, away from moisture and light |
| 酸度系数(pKa) | 10.17±0.10(Predicted) |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
Patamostat (E-3123) 是一种有效的蛋白酶 (protease) 抑制剂。Patamostat 有效抑制胰蛋白酶，纤溶酶和凝血酶，IC50 分别为 39 nM，950 nM 和 1.9 μM。Patamostat 有潜力用于急性胰腺炎的研究。
IC50: 39 nM (trypsin), 950 nM (plasmin) and 1.9 μM (thrombin)
Intravenous infusion of Patamostat (E-3123) at 0.03-0.3 mg/kg in rats or at 0.3-3.0 mg/kg in rabbits reduced mortality after the induction of pancreatitis in a dose-dependent manner. In dogs with pancreatitis, increases in serum trypsin and lipase activities were significantly reduced by infusion of Patamostat at 1.0 and 3.0 mg/kg.
Patamostat (E3123; continuous infusion in a dose of 2 mg/kg per h) improves almost all parameters, including mortality rate, serum and ascitic fluid amylase levels, plasma endotoxin and serum FDP levels, and distribution of lysosomal enzyme in male Wistar rats.
| Animal Model: | Male Wistar rats weighing about 350 g |
| Dosage: | 2 mg/kg |
| Administration: | Continuous infusion per h for 1 h |
| Result: | Significantly improved the survival rate. |