| CAS NO: | 2271122-53-1 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| Cas No. | 2271122-53-1 |
| Canonical SMILES | CC1=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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation 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. |
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