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114568-32-0

114568-32-0 structure
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
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 structure

55943-72-1

~%

114568-32-0 structure

114568-32-0
Literature: Nochi; Shimomura; Hattori; Sato; Miyake; Tanizawa Chemical and Pharmaceutical Bulletin, 1989 , vol. 37, # 10 p. 2855 - 2857
114568-48-8 structure

114568-48-8

~%

114568-32-0 structure

114568-32-0
Literature: Nochi; Shimomura; Hattori; Sato; Miyake; Tanizawa Chemical and Pharmaceutical Bulletin, 1989 , vol. 37, # 10 p. 2855 - 2857
75-75-2 structure

75-75-2
114568-26-2 structure

114568-26-2

~%

114568-32-0 structure

114568-32-0
Literature: Nochi; Shimomura; Hattori; Sato; Miyake; Tanizawa Chemical and Pharmaceutical Bulletin, 1989 , vol. 37, # 10 p. 2855 - 2857
Precursor  4

DownStream  0


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