114568-32-0

114568-32-0 structure

Name: Patomostat mesilate
Chemical Name: [4-[2-(2,5-dioxopyrrolidin-1-yl)ethylsulfanyl]phenyl] 4-(diaminomethylideneamino)benzoate,methanesulfonic acid
CAS Number: 114568-32-0
Molecular Formula: C₂₁H₂₄N₄O₇S₂
Molecular Weight: 508.56800
Catalog: Signaling Pathways Metabolic Enzyme/Protease Ser/Thr Protease
Create Date: 2017-04-04 10:20:14
Modify Date: 2024-01-10 20:02:02
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
Synonyms	Patamostat mesylate Patamostat mesilate

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.

Molecular Formula	C₂₁H₂₄N₄O₇S₂
Molecular Weight	508.56800
Exact Mass	508.10900
PSA	213.63000
LogP	3.84800

Hazard Codes	Xi

55943-72-1

114568-32-0

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

114568-48-8

114568-32-0

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

75-75-2

114568-26-2

114568-32-0

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

Precursor 4
55943-72-1 114568-48-8 75-75-2 114568-26-2
DownStream 0

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