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ChemicalBook  CAS数据库列表  4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate

4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate

生物活性 靶点 体内研究
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
  • 中文名:4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate
  • 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)
  • 形态 :Solid
  • 颜色 :White to off-white

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.
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