1. Metabolic Enzyme/Protease
  2. PAI-1

ZK824859 

Cat. No.: HY-114330
Handling Instructions

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.

For research use only. We do not sell to patients.

ZK824859 Chemical Structure

ZK824859 Chemical Structure

CAS No. : 2271122-53-1

Size Price Stock
5 mg USD 450 Get quote
10 mg USD 750 Get quote
50 mg USD 2100 Get quote
100 mg USD 3300 Get quote

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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].

IC50 & 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 (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].

Animal Model: Female SJL mice with chronic mouse EAE model[1]
Dosage: 50, 25 and 10 mg/kg
Administration: B.i.d.; 25 days
Result: Prevented the development of disease at 50 mg/kg completely. However, 25 and 10 mg/kg had no effect on clinical scores.
References
Molecular Weight

428.43

Formula

C₂₃H₂₂F₂N₂O₄

CAS No.

2271122-53-1

SMILES

CC1=CC(OC2=C(F)C=C(F)C(O[[email protected]](CC)C(O)=O)=N2)=CC(C3=CC=CC(CN)=C3)=C1

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
ZK824859
Cat. No.:
HY-114330
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ZK824859

Cat. No.: HY-114330