Patomostat mesilate

Modify Date: 2024-01-10 20:02:02

Patomostat mesilate structure	Common Name	Patomostat mesilate
	CAS Number	114568-32-0	Molecular Weight	508.56800
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₁H₂₄N₄O₇S₂	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Patomostat mesilate

Patamostat (E-3123) mesylate is a potent protease inhibitor. Patamostat mesylate potently inhibits trypsin, plasmin and thrombin with IC50s of 39 nM, 950 nM and 1.9 μM, respectively. Patamostat mesylate 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,methanesulfonic acid
Synonym	More Synonyms

Description	Patamostat (E-3123) mesylate is a potent protease inhibitor. Patamostat mesylate potently inhibits trypsin, plasmin and thrombin with IC50s of 39 nM, 950 nM and 1.9 μM, respectively. Patamostat mesylate 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	Patamostat mesylate (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 mesylate (1.0-3.0 mg/kg; intravenous infusion) reduces the increases of serum trypsin and lipase activities in dogs with pancreatitis[1]. Patamostat mesylate (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.
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.