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编 号：F282828
分子式：C23H22F2N2O4
分子量：428.43
分子式：C23H22F2N2O4
分子量：428.43
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CAS No: 2271122-53-1
产品详情
生物活性：
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.
体内研究：
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.Animal Model:Female SJL mice with chronic mouse EAE model
Dosage:50, 25 and 10?mg/kg
Administration:B.i.d.; 25 days
Result:Prevented the development of disease at50?mg/kg completely. However, 25 and 10?mg/kg had no effect on clinical scores.
体外研究：
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.
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.
体内研究：
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.Animal Model:Female SJL mice with chronic mouse EAE model
Dosage:50, 25 and 10?mg/kg
Administration:B.i.d.; 25 days
Result:Prevented the development of disease at50?mg/kg completely. However, 25 and 10?mg/kg had no effect on clinical scores.
体外研究：
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.
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