ZK824190

Names

[ Name ]:
ZK824190

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> PAI-1

Signaling Pathways >> Metabolic Enzyme/Protease >> Ser/Thr Protease

Research Areas >> Inflammation/Immunology

[Target]

IC50: 237 nM (uPA), 1600 nM (tPA), 1850 nM (Plasmin)[1]

[In Vivo]

ZK824190 (2 mg/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: 2 mg/kg (Pharmacokinetic Analysis) Administration: PO Result: Oral availability F = 55%; Cmax= 0.64 g/mL and AUC = 2.2 h*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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₂H₂₀F₂N₂O₄

[ Molecular Weight ]:
428.44

[ Storage condition ]:
Store at 4-8°C

Related Compounds

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