1. Metabolic Enzyme/Protease
  2. Ser/Thr Protease
    PAI-1
  3. ZK824190

ZK824190 

Cat. No.: HY-126361
Handling Instructions

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.

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

ZK824190 Chemical Structure

ZK824190 Chemical Structure

CAS No. : 2254001-81-3

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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].

IC50 & 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

414.40

Formula

C22H20F2N2O4

CAS No.
SMILES

CC[[email protected]@H](OC1=NC(OC2=CC(C3=CC=CC(CN)=C3)=CC=C2)=C(F)C=C1F)C(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (603.28 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4131 mL 12.0656 mL 24.1313 mL
5 mM 0.4826 mL 2.4131 mL 4.8263 mL
10 mM 0.2413 mL 1.2066 mL 2.4131 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.08 mg/mL (5.02 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (5.02 mM); Clear solution

*All of the co-solvents are available by MCE.
References
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Product Name:
ZK824190
Cat. No.:
HY-126361
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