CZC-54252
Based on 1 Customer Validation
CZC-54252 is a potent and selective LRRK2 inhibitor with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2, respectively. CZC-54252 attenuates G2019S LRRK2-induced human neuronal injury with an EC50 of ~1 nM. CZC-54252 has a neuroprotective activity.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.05%
- CAS. Nr.: 1191911-27-9
- Formel: C22H25ClN6O4S
- Molecular Weight:504.99
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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
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Biologische Aktivität
IC50: 1.28 nM (Wild-type LRRK2) and 1.85 nM (G2019S LRRK2)[1]
CZC-54252 inhibits the activity of recombinant human wild-type LRRK2 with an IC50 ranging from ～1 to ～5 nM. In addition, they are screened against a kinase panel of 185 kinases and exhibited good selectivity[1].
G2019S LRRK2-induced human neuronal injury is attenuated by CZC-54252 with an EC50 of ~1 nM and fully reversed to wild-type levels by CZC-54252 at concentration of 1.6 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1191911-27-9
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Appearance Solid
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Molecular Weight 504.99
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Formel C22H25ClN6O4S
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Color White to off-white
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SMILES
CS(=O)(NC1=CC=CC=C1NC2=NC(NC3=CC=C(N4CCOCC4)C=C3OC)=NC=C2Cl)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Lösungsmittel & Löslichkeit
DMSO : ≥ 100 mg/mL (198.02 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.5 mg/mL (4.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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
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Data Sheet (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9802 mL | 9.9012 mL | 19.8024 mL | 49.5059 mL |
| 5 mM | 0.3960 mL | 1.9802 mL | 3.9605 mL | 9.9012 mL | |
| 10 mM | 0.1980 mL | 0.9901 mL | 1.9802 mL | 4.9506 mL | |
| 15 mM | 0.1320 mL | 0.6601 mL | 1.3202 mL | 3.3004 mL | |
| 20 mM | 0.0990 mL | 0.4951 mL | 0.9901 mL | 2.4753 mL | |
| 25 mM | 0.0792 mL | 0.3960 mL | 0.7921 mL | 1.9802 mL | |
| 30 mM | 0.0660 mL | 0.3300 mL | 0.6601 mL | 1.6502 mL | |
| 40 mM | 0.0495 mL | 0.2475 mL | 0.4951 mL | 1.2376 mL | |
| 50 mM | 0.0396 mL | 0.1980 mL | 0.3960 mL | 0.9901 mL | |
| 60 mM | 0.0330 mL | 0.1650 mL | 0.3300 mL | 0.8251 mL | |
| 80 mM | 0.0248 mL | 0.1238 mL | 0.2475 mL | 0.6188 mL | |
| 100 mM | 0.0198 mL | 0.0990 mL | 0.1980 mL | 0.4951 mL |
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