ZK824190
Based on 1 publication(s) in Google Scholar
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 2254001-81-3
- Formel: C22H20F2N2O4
- Molecular Weight:414.40
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) ZK824190
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Biologische Aktivität
IC50: 237 nM (uPA), 1600 nM (tPA), 1850 nM (Plasmin)[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats with experimental autoimmune encephalomyelitis (EAE) model[1]
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Dosage:2 mg/kg (Pharmacokinetic Analysis)
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Administration:PO
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Result:Oral availability F = 55%; Cmax= 0.64 g/mL and AUC = 2.2 h*g/mL; T1/2=2.8 h.
Chemical Information
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CAS. Nr. 2254001-81-3
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Molecular Weight 414.40
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Formel C22H20F2N2O4
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SMILES
CC[C@@H](OC1=NC(OC2=CC(C3=CC=CC(CN)=C3)=CC=C2)=C(F)C=C1F)C(O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Bioorg Chem
Identification of FTY720 and COH29 as novel topoisomerase I catalytic inhibitors by experimental and computational studies. [Abstract]2024 Jun:147:107412. PMID: 38696845
Lösungsmittel & Löslichkeit
DMSO : 250 mg/mL (603.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
Verweise
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4131 mL | 12.0656 mL | 24.1313 mL | 60.3282 mL |
| 5 mM | 0.4826 mL | 2.4131 mL | 4.8263 mL | 12.0656 mL | |
| 10 mM | 0.2413 mL | 1.2066 mL | 2.4131 mL | 6.0328 mL | |
| 15 mM | 0.1609 mL | 0.8044 mL | 1.6088 mL | 4.0219 mL | |
| 20 mM | 0.1207 mL | 0.6033 mL | 1.2066 mL | 3.0164 mL | |
| 25 mM | 0.0965 mL | 0.4826 mL | 0.9653 mL | 2.4131 mL | |
| 30 mM | 0.0804 mL | 0.4022 mL | 0.8044 mL | 2.0109 mL | |
| 40 mM | 0.0603 mL | 0.3016 mL | 0.6033 mL | 1.5082 mL | |
| 50 mM | 0.0483 mL | 0.2413 mL | 0.4826 mL | 1.2066 mL | |
| 60 mM | 0.0402 mL | 0.2011 mL | 0.4022 mL | 1.0055 mL | |
| 80 mM | 0.0302 mL | 0.1508 mL | 0.3016 mL | 0.7541 mL | |
| 100 mM | 0.0241 mL | 0.1207 mL | 0.2413 mL | 0.6033 mL |
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