ZK824859是一种口服有效的选择性尿激酶型纤溶酶原激活剂(uPA)抑制剂，用于人uPA，tPA和纤溶酶，IC50分别为79nM，1580nM和1330nM。
CAS：2271122-53-1
分子式：C23H22F2N2O4
分子量：428.43
纯度：98%
存储：Store at -20°C

Background:

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].

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].

ZK824859 shows efficacy in acute and chronic EAE model for multiple sclerosis. In a chronic mouse EAE model at a dose of 50?mg/kg b.i.d. ZK824859 completely prevents the development of disease. However, two lower doses (25 and 10?mg/kg) have no effect on clinical scores. In an acute mouse EAE model, ZK824859 is also efficacious. In this study the 50 and 25?mg/kg b.i.d. doses show a reduction in clinical scores compared to the control group, although only the 25?mg/kg treatment regime is statistically significant compared to the control group[1].

[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.