2254001-81-3

2254001-81-3 structure

Name: ZK824190
Chemical Name: ZK824859
CAS Number: 2254001-81-3
Molecular Formula: C₂₂H₂₀F₂N₂O₄
Molecular Weight: 428.44
Catalog: Signaling Pathways Metabolic Enzyme/Protease PAI-1
Create Date: 2019-09-07 19:06:18
Modify Date: 2024-01-08 10:43:30
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].

Name	ZK824859

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.