114568-26-2

Name	4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate
CAS	114568-26-2
Molecular Formula	C20H20N4O4S
MDL Number	MFCD00868441
Molecular Weight	412.46
MOL File	114568-26-2.mol

Synonyms

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

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Chemical Properties

Melting point	201.6 °C
Boiling point	653.2±65.0 °C(Predicted)
density	1.41±0.1 g/cm3(Predicted)
storage temp.	4°C, away from moisture and light
form	Solid
pka	10.17±0.10(Predicted)
color	White to off-white

Hazard Information

Uses

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. Patamostat may possess suppressing effects on pathogenesis and development of acute pancreatitis[1][2].

in vivo

Patamostat (intravenous infusion) at 0.03-0.3 mg/kg in rats or at 0.3-3.0 mg/kg in rabbits reduces mortality after the induction of pancreatitis in a dose-dependent manner^[1].
Patamostat (1.0-3.0 mg/kg; intravenous infusion) reduces the increases of serum trypsin and lipase activities in dogs with pancreatitis^[1].
Patamostat (2 mg/kg per h; continuous infusion) 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.

storage

4°C, away from moisture and light

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. DOI:10.1254/fpj.91.285
[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. DOI:10.1111/j.1440-1746.1993.tb01175.x

Supplier

TargetMol Chemicals Inc.

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