ZK824859 

ZK824859 is an oral available and selective urokinase plasminogen activator (uPA) inhibitor with IC₅₀s 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 IC₅₀ values of 79 nM, 1580 nM and 1330 nM respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

428.43

C₂₃H₂₂F₂N₂O₄

2271122-53-1

CC1=CC(OC2=C(F)C=C(F)C(O[C@H](CC)C(O)=O)=N2)=CC(C3=CC=CC(CN)=C3)=C1

Room temperature in continental US; may vary elsewhere.

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

• [1]. Islam I, et al. Discovery of selective urokinase plasminogen activator (uPA) inhibitors as a potential treatment for multiple sclerosis. Bioorg Med Chem Lett. 2018 Nov 1;28(20):3372-3375.  [Content Brief]