ZK824859 is an oral available and selective urokinase plasminogen activator (uPA) inhibitor withIC₅₀s of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively^[1].

IC50: 79 nM (human uPA), 1580 nM (human tPA), 1330 nM (human plasmin)^[1].

ZK824859 is 5 fold less potent and has lost selectivity in mouse: uPA IC₅₀=410 nM; tPA IC₅₀=910 nM; plasmin IC₅₀=1600 nM compared to human IC₅₀values of 79 nM, 1580 nM and 1330 nM respectively^[1].

ZK824859 (50, 25 and 10 mg/kg; b.i.d.; 25 days) is used in a chronic mouse EAE model. ZK 824859 completely prevents the development of disease. However, two lower doses (25 and 10 mg/kg) have no effect on clinical scores^[1].

428.43

C₂₃H₂₂F₂N₂O₄

2271122-53-1

Room temperature in continental US; may vary elsewhere.

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