| Identification | Back Directory | [Name]
4-(2-succinimidoethylthio)phenyl 4-guanidinobenzoate | [CAS]
114568-26-2 | [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 | [Molecular Formula]
C20H20N4O4S | [MDL Number]
MFCD00868441 | [MOL File]
114568-26-2.mol | [Molecular Weight]
412.46 |
| Chemical Properties | Back Directory | [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 | Back Directory | [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 |
|
| Company Name: |
MedChemExpress
|
| Tel: |
021-58955995 |
| Website: |
www.medchemexpress.com |
|