Patamostat mesylate  (Synonyms: E-3123 mesylate)

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].

IC50: 39 nM (trypsin), 950 nM (plasmin) and 1.9 μM (thrombin)^[1]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

508.57

C₂₁H₂₄N₄O₇S₂

114568-32-0

O=C(OC1=CC=C(SCCN2C(CCC2=O)=O)C=C1)C3=CC=C(NC(N)=N)C=C3.CS(O)(=O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]