For research use only. Not for therapeutic Use.
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[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 (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[1].
| Catalog Number | I046242 |
| CAS Number | 2436760-76-6 |
| Synonyms | (2R)-2-[6-[3-[3-(aminomethyl)phenyl]-5-methylphenoxy]-3,5-difluoropyridin-2-yl]oxybutanoic acid;hydrochloride |
| Molecular Formula | C23H23ClF2N2O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C23H22F2N2O4.ClH/c1-3-20(23(28)29)31-22-19(25)11-18(24)21(27-22)30-17-8-13(2)7-16(10-17)15-6-4-5-14(9-15)12-26;/h4-11,20H,3,12,26H2,1-2H3,(H,28,29);1H/t20-;/m1./s1 |
| InChIKey | XACCKEPNGBUXQW-VEIFNGETSA-N |
| SMILES | CCC(C(=O)O)OC1=C(C=C(C(=N1)OC2=CC(=CC(=C2)C3=CC=CC(=C3)CN)C)F)F.Cl |
| Reference | [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. |
