1. Metabolic Enzyme/Protease
  2. PAI-1

ZK824859 hydrochloride 

Cat. No.: HY-114330A
Handling Instructions

ZK824859 hydrochloride 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 hydrochloride Chemical Structure

ZK824859 hydrochloride Chemical Structure

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 495 In-stock
Estimated Time of Arrival: December 31
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 750 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3300 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Other Forms of ZK824859 hydrochloride:

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

ZK824859 hydrochloride 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: 

DMSO : ≥ 125 mg/mL (268.88 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1510 mL 10.7552 mL 21.5105 mL
5 mM 0.4302 mL 2.1510 mL 4.3021 mL
10 mM 0.2151 mL 1.0755 mL 2.1510 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution

References
Molecular Weight

464.89

Formula

C₂₃H₂₃ClF₂N₂O₄

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.Cl

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

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Product Name:
ZK824859 hydrochloride
Cat. No.:
HY-114330A
Quantity:

ZK824859 hydrochloride

Cat. No.: HY-114330A