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4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate

4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate, 114568-26-2, 结构式
4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate
CAS号:
114568-26-2
英文名:
4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate
英文别名:
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
中文名:
4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate
中文别名:
化合物 PATAMOSTAT
CBNumber:
CB31373166
分子式:
C20H20N4O4S
分子量:
412.46
MOL File:
114568-26-2.mol

4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate化学性质

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)
安全信息

4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate性质、用途与生产工艺

生物活性

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。

靶点

IC50: 39 nM (trypsin), 950 nM (plasmin) and 1.9 μM (thrombin)

体内研究

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.

4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate 上下游产品信息

上游原料

下游产品


4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate 生产厂家

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天津普西唐生物医药科技有限公司 010-60605840 psaitong@jm-bio.com 中国 29778 58
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銳迪國際科技有限公司 18024082417 market@ubiochem.com 中国 9154 58
 

114568-26-2, 4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate 相关搜索:

  • 化合物 PATAMOSTAT
  • 114568-26-2
  • Benzoic acid, 4-[(aminoiminomethyl)amino]-, 4-[[2-(2,5-dioxo-1-pyrrolidinyl)ethyl]thio]phenyl ester
  • Patomostat
  • 4-Guanidinobenzoic acid 4-[[2-(2,5-dioxopyrrolidin-1-yl)ethyl]thio]phenyl ester
  • 4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate
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