4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate
中文名称 | 4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate |
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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 |
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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 |
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. |