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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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

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 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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3341 mL 11.6705 mL 23.3410 mL
5 mM 0.4668 mL 2.3341 mL 4.6682 mL
10 mM 0.2334 mL 1.1671 mL 2.3341 mL
*Please refer to the solubility information to select the appropriate solvent.
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