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编 号:F752735
分子式:C23H23ClF2N2O4
分子量:464.89
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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生物活性:
ZK824859 hydrochloride 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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