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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 114568-26-2 結(jié)構(gòu)式

基本信息

中文別名
化合物 PATAMOSTAT
英文別名
Patomostat
4-(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(diǎn)201.6 °C
沸點(diǎn)653.2±65.0 °C(Predicted)
密度1.41±0.1 g/cm3(Predicted)
儲(chǔ)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(diǎn)

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.
"114568-26-2" 相關(guān)產(chǎn)品信息
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