| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
uPA (IC50 = 237 nM); tPA (IC50 = 1600 nM); Plasmin (IC50 = 1850 nM)
Urokinase plasminogen activator (uPA). ZK824190 also inhibits tissue plasminogen activator (tPA) and plasmin with lower potency. The compound's selectivity for uPA makes it a valuable tool for studying the role of the uPA system in various diseases. |
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| ln Vitro |
ZK824190 inhibits uPA with an IC50 of 237 nM, tPA with an IC50 of 1600 nM, and plasmin with an IC50 of 1850 nM. This selectivity profile demonstrates that the compound is a more potent inhibitor of uPA compared to related serine proteases.
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| ln Vivo |
ZK824190 (2 mg/kg; PO) has a half-life of 2.8 hours and a comparatively high oral availability[1].
ZK824190 has been investigated as a potential treatment for multiple sclerosis. Its oral bioavailability supports its potential for therapeutic use in chronic diseases. The compound's mechanism of action involves the inhibition of uPA-mediated processes. |
| Enzyme Assay |
Enzyme inhibition assays are performed using recombinant uPA, tPA, and plasmin enzymes. ZK824190 is incubated with the enzymes and substrates, and the inhibition of protease activity is measured. IC50 values are determined from dose-response curves.
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| Cell Assay |
Cell-based assays for ZK824190 would involve the evaluation of uPA-mediated processes in various cell types. The compound's ability to inhibit uPA activity and downstream signaling pathways would be assessed. However, specific cell-based assay details are not extensively reported.
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| Animal Protocol |
Rats with experimental autoimmune encephalomyelitis (EAE) model[1]
2 mg/kg (Pharmacokinetic Analysis) PO In vivo efficacy of ZK824190 has been evaluated in animal models of multiple sclerosis. The compound is administered orally, and its effects on disease progression and neuroinflammation are assessed. These studies support its potential as a therapeutic agent. |
| ADME/Pharmacokinetics |
ZK824190 is orally bioavailable, supporting its potential for therapeutic use. The compound's favorable PK properties make it suitable for chronic administration in preclinical studies. Detailed PK parameters would require further investigation from primary literature.
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| Toxicity/Toxicokinetics |
Toxicity data for ZK824190 are not extensively reported in the available literature. The compound is intended for research use only. Its investigation as a potential treatment for multiple sclerosis suggests it has an acceptable safety profile in preclinical studies.
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| References | |
| Additional Infomation |
ZK824190 is a research compound being investigated as a potential treatment for multiple sclerosis. It is an orally available and selective uPA inhibitor. The compound is not approved for clinical use and is supplied for research purposes only.
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| Molecular Formula |
C23H22F2N2O4
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|---|---|
| Molecular Weight |
428.428593158722
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| Exact Mass |
428.15
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| Elemental Analysis |
C, 64.48; H, 5.18; F, 8.87; N, 6.54; O, 14.94
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| CAS # |
2254001-81-3
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| Related CAS # |
ZK824190 hydrochloride;2629177-12-2
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| PubChem CID |
69496820
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| Appearance |
Solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
31
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| Complexity |
584
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| Defined Atom Stereocenter Count |
1
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| InChi Key |
CVNXUNVHFJANHX-HXUWFJFHSA-N
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| InChi Code |
InChI=1S/C23H22F2N2O4/c1-3-20(23(28)29)31-22-19(25)11-18(24)21(27-22)30-17-8-13(2)7-16(10-17)15-6-4-5-14(9-15)12-26/h4-11,20H,3,12,26H2,1-2H3,(H,28,29)/t20-/m1/s1
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| Chemical Name |
(2R)-2-[6-[3-[3-(aminomethyl)phenyl]-5-methylphenoxy]-3,5-difluoropyridin-2-yl]oxybutanoic acid
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| Synonyms |
ZK-824190; ZK 824190; ZK824859
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~86 mg/mL (~207.5 mM)
Ethanol: ~86 mg/mL (~207.5 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.02 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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