ZK824859 hydrochloride (C09-1186-005)

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.IC50& Target:IC50: 79 nM (human uPA), 1580 nM (human tPA), 1330 nM (human plasmin) .In Vitro: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. MCE has not independently confirmed the accuracyIn Vivo:ZK824859 (50, 25 and 10mg/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 10mg/kg) have no effect on clinical scores. MCE has not independently coBiological Activity:ZK824859 hydrochloride is an oral available and selective urokinase plasminogen activator ( uPA ) inhibitor with IC 50 s of 79u202fnM, 1580u202fnM and 1330u202fnM for human uPA, tPA, and plasmin, respectively. Specifications and Purity: 10mM in DMSO. Molecular Formula: C23H23ClF2N2O4. Molecular Weight: 464.89.