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114568-26-2

114568-26-2 structure
114568-26-2 structure
  • Name: Patamostat
  • Chemical Name: [4-[2-(2,5-dioxopyrrolidin-1-yl)ethylsulfanyl]phenyl] 4-(diaminomethylideneamino)benzoate
  • CAS Number: 114568-26-2
  • Molecular Formula: C20H20N4O4S
  • Molecular Weight: 412.46200
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease Ser/Thr Protease
  • Create Date: 2018-06-22 19:48:00
  • Modify Date: 2024-01-10 13:29:11
  • Patamostat (E-3123) is a potent protease inhibitor. Patamostat potently inhibits trypsin, plasmin and thrombin with IC50s of 39 nM, 950 nM and 1.9 μM, respectively. E-3123 may possess suppressing effects on pathogenesis and development of acute pancreatitis[1][2].

Name [4-[2-(2,5-dioxopyrrolidin-1-yl)ethylsulfanyl]phenyl] 4-(diaminomethylideneamino)benzoate
Synonyms Patamostat
p-((2-Succinimidoethyl)thio)phenyl p-guanidinobenzoate
Benzoic acid,4-((aminoiminomethyl)amino)-,4-((2-(2,5-dioxo-1-pyrrolidinyl)ethyl)thio)phenyl ester
Patamostat [INN]
E 3123
4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate
UNII-2T7W4EA51W
Description Patamostat (E-3123) is a potent protease inhibitor. Patamostat potently inhibits trypsin, plasmin and thrombin with IC50s of 39 nM, 950 nM and 1.9 μM, respectively. E-3123 may possess suppressing effects on pathogenesis and development of acute pancreatitis[1][2].
Related Catalog
Target

IC50: 39 nM (trypsin), 950 nM (plasmin) and 1.9 μM (thrombin)[1]

In Vivo 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[1]. 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[2]. Animal Model: Male Wistar rats weighing about 350 g[2] Dosage: 2 mg/kg Administration: Continuous infusion per h for 1 h Result: Significantly improved the survival rate.
References

[1]. K Miyamoto, et al. [Effects of E-3123, a New Protease Inhibitor, on Several Protease Activities and on Experimental Acute Pancreatitis]. Nihon Yakurigaku Zasshi. 1988 May;91(5):285-93.

[2]. T Hirano, et al. Protective Effect of a Cephalosporin, Shiomarin, Plus a New Potent Protease Inhibitor, E3123, on Rat Taurocholate-Induced Pancreatitis. J Gastroenterol Hepatol. Jan-Feb 1993;8(1):52-9.

Density 1.41g/cm3
Boiling Point 701.5ºC at 760mmHg
Molecular Formula C20H20N4O4S
Molecular Weight 412.46200
Flash Point 378.1ºC
Exact Mass 412.12100
PSA 150.88000
LogP 3.26320
Vapour Pressure 1.58E-19mmHg at 25°C
Index of Refraction 1.678
Hazard Codes Xi

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114568-26-2 structure

114568-26-2

Literature: Nochi; Shimomura; Hattori; Sato; Miyake; Tanizawa Chemical and Pharmaceutical Bulletin, 1989 , vol. 37, # 10 p. 2855 - 2857