[CAS NO. 2436760-76-6] ZK824859hydrochloride
PRODUCTS SPECIFICATIONS [2436760-76-6]
DESCRIPTION [2436760-76-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 464.89 |
| Molecular Formula | C23H23ClF2N2O4 |
| SMILES | CC1=CC(OC2=C(F)C=C(F)C(O[C@H](CC)C(O)=O)=N2)=CC(C3=CC=CC(CN)=C3)=C1.Cl |
Summary
ZK824859 hydrochloride is an oral available and selective urokinase plasminogen activator ( uPA ) inhibitor with IC 50 s 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 IC 50 =410 nM; tPA IC 50 =910 nM; plasmin IC 50 =1600 nM compared to human IC 50 values of 79 nM, 1580 nM and 1330 nM respectively [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : ≥ 125 mg/mL ( 268.88 mM )
* "≥" means soluble, but saturation unknown.
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 |
