ZK824859 hydrochloride 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 79 nM，1580 nM 和 1330 nM。

ZK824859 hydrochloride is an oral available and selective urokinase plasminogen activator ( uPA ) inhibitor with IC 50 s 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 IC 50 =410 nM; tPA IC 50 =910 nM; plasmin IC 50 =1600 nM compared to human IC 50 values 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]. Animal Model: Female SJL mice with chronic mouse EAE model [1] Dosage: 50, 25 and 10 mg/kg Administration: B.i.d.; 25 days Result: Prevented the development of disease at 50 mg/kg completely. However, 25 and 10 mg/kg had no effect on clinical scores.

C23H23ClF2N2O4

464.89

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years