<Suppliers Price>

Patamostat

Names

[ CAS No. ]:
114568-26-2

[ 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