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ZK824859
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ZK824859图片
CAS NO:2271122-53-1
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
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 No.2271122-53-1
Canonical SMILESCC1=CC(OC2=C(F)C=C(F)C(O[C@H](CC)C(O)=O)=N2)=CC(C3=CC=CC(CN)=C3)=C1
分子式C23H22F2N2O4
分子量428.43
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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 50mg/kg b.i.d. ZK824859 completely prevents the development of disease. However, two lower doses (25 and 10mg/kg) have no effect on clinical scores. In an acute mouse EAE model, ZK824859 is also efficacious. In this study the 50 and 25mg/kg b.i.d. doses show a reduction in clinical scores compared to the control group, although only the 25mg/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.