Patamostat

Names

[ Name ]:
Patamostat

[Synonym ]:
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

Biological Activity

[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]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Ser/Thr Protease

Research Areas >> Inflammation/Immunology

[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.

Chemical & Physical Properties

[ 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

Safety Information

[ Hazard Codes ]:
Xi

Synthetic Route

Click to get detail synthetic route

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.