2271122-53-1

2271122-53-1 structure

Name: ZK824859
Chemical Name: ZK824859
CAS Number: 2271122-53-1
Molecular Formula: C₂₃H₂₂F₂N₂O₄
Molecular Weight: 428.43
Catalog: Signaling Pathways Metabolic Enzyme/Protease PAI-1
Create Date: 2019-03-03 11:36:02
Modify Date: 2024-01-11 18:45:10
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].

Name	ZK824859

Description	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].
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> PAI-1 Research Areas >> Inflammation/Immunology
Target	IC50: 79 nM (human uPA), 1580 nM (human tPA), 1330 nM (human plasmin)[1].
In Vitro	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].
In Vivo	ZK824859 shows efficacy in acute and chronic EAE model for multiple sclerosis. In a chronic mouse EAE model at a dose of 50 mg/kg b.i.d. ZK824859 completely prevents the development of disease. However, two lower doses (25 and 10 mg/kg) have no effect on clinical scores. In an acute mouse EAE model, ZK824859 is also efficacious. In this study the 50 and 25 mg/kg b.i.d. doses show a reduction in clinical scores compared to the control group, although only the 25 mg/kg treatment regime is statistically significant compared to the control group[1].
References	[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.