Patamostat (E-3123) is a potent protease inhibitor. Patamostat potently inhibits trypsin, plasmin and thrombin with IC 50 s of 39 nM, 950 nM and 1.9 μM, respectively. Patamostat may possess suppressing effects on pathogenesis and development of acute pancreatitis 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 . Patamostat (1.0-3.0 mg/kg; intravenous infusion) reduces the increases of serum trypsin and lipase activities in dogs with pancreatitis . 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Wistar rats weighing about 350 gDosage: 2 mg/kg Administration: Continuous infusion per h for 1 h Result: Significantly improved the survival rate. Form:Solid IC50& Target:IC50: 39 nM (trypsin), 950 nM (plasmin) and 1.9 μM (thrombin)
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Patamostat
CAS number:114568-26-2 molecular formula:C20H20N4O4S
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| Chinese alias | 帕塔莫司他 | ||
| English alias | Patamostat [INN] | Q27255575 | p-((2-Succinimidoethyl)thio)phenyl p-guanidinobenzoate | UNII-2T7W4EA51W | Benzoic acid, 4-((aminoiminomethyl)amino)-, 4-((2-(2,5-dioxo-1-pyrrolidinyl)ethyl)thio)phenyl ester | SCHEMBL2109248 | DTXSID90150785 | 2T7W4EA51W | | ||
| CAS number | 114568-26-2 | molecular formula | C20H20N4O4S |
| molecular weight | 412.46 g/mol | Exact mass | ≥99% |
| PSA | 153.000 Ų | logp | 1.2 |
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