1. Metabolic Enzyme/Protease
  2. Ser/Thr Protease
  3. Patamostat

Patamostat (Synonyms: E-3123)

Cat. No.: HY-114080
Handling Instructions

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. E-3123 may possess suppressing effects on pathogenesis and development of acute pancreatitis.

For research use only. We do not sell to patients.

Patamostat Chemical Structure

Patamostat Chemical Structure

CAS No. : 114568-26-2

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Description

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. E-3123 may possess suppressing effects on pathogenesis and development of acute pancreatitis[1][2].

IC50 & Target

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

In Vivo

Intravenous infusion of Patamostat (E-3123) at 0.03-0.3 mg/kg in rats or at 0.3-3.0 mg/kg in rabbits reduced mortality after the induction of pancreatitis in a dose-dependent manner. In dogs with pancreatitis, increases in serum trypsin and lipase activities were significantly reduced by infusion of Patamostat at 1.0 and 3.0 mg/kg[1].
Patamostat (E3123; continuous infusion in a dose of 2 mg/kg per h) 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.
Molecular Weight

412.46

Formula

C₂₀H₂₀N₄O₄S

CAS No.

114568-26-2

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

PatamostatE-3123E3123E 3123Ser/Thr ProteaseSerine proteasesSerine endopeptidasesThreonine proteasesproteasetrypsinplasminthrombinpathogenesisacutepancreatitisInhibitorinhibitorinhibit

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Patamostat
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HY-114080
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