114568-26-2
中文名稱
4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate
英文名稱
4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate
CAS
114568-26-2
分子式
C20H20N4O4S
分子量
412.46
MOL 文件
114568-26-2.mol
114568-26-2 結(jié)構(gòu)式
基本信息
中文別名
化合物 PATAMOSTAT 英文別名
Patomostat4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate
4-Guanidinobenzoic acid 4-[[2-(2,5-dioxopyrrolidin-1-yl)ethyl]thio]phenyl ester
Benzoic acid, 4-[(aminoiminomethyl)amino]-, 4-[[2-(2,5-dioxo-1-pyrrolidinyl)ethyl]thio]phenyl ester
物理化學(xué)性質(zhì)
熔點201.6 °C
沸點653.2±65.0 °C(Predicted)
密度1.41±0.1 g/cm3(Predicted)
儲存條件4°C, away from moisture and light
酸度系數(shù)(pKa)10.17±0.10(Predicted)
形態(tài)Solid
顏色White to off-white
常見問題列表
生物活性
Patamostat (E-3123) 是一種有效的蛋白酶 (protease) 抑制劑。Patamostat 有效抑制胰蛋白酶，纖溶酶和凝血酶，IC50 分別為 39 nM，950 nM 和 1.9 μM。Patamostat 有潛力用于急性胰腺炎的研究。靶點
IC50: 39 nM (trypsin), 950 nM (plasmin) and 1.9 μM (thrombin)
體內(nèi)研究
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. |