ZK824190 is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis. IC50s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively[1].
in vivo
ZK824190 (2mg/kg; PO) exhibits a relatively high oral availability and a moderate half time (T1/2=2.8 h)[1].
Animal Model:
Rats with experimental autoimmune encephalomyelitis (EAE) model[1]
Dosage:
2mg/kg (Pharmacokinetic Analysis)
Administration:
PO
Result:
Oral availability F=55%; Cmax=0.64g/mL and AUC=2.2h*g/mL; T1/2=2.8 h.
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. DOI:10.1016/j.bmcl.2018.09.001
