EB-42486
Based on 1 Customer Validation
EB-42486 is a novel, potent, and highly selective G2019S-LRRK2 inhibitor (IC50: < 0.2 nM). EB-42486 can be used in the research of Parkinson's disease.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.62%
- No. CAS: 2390475-81-5
- Fòrmula: C22H22N8O
- Peso molecular:414.46
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
Chemical Information
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No. CAS 2390475-81-5
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Appearance Solid
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Peso molecular 414.46
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Fòrmula C22H22N8O
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Color Off-white to light yellow
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SMILES
O=C(C1=C(C)N(C)C2=NN=NN2C1(C)C)NC3=CC4=C(NN=C4C5=CC=CC=C5)C=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 125 mg/mL (301.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (5.02 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
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.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (604 KB)
- English - EN (604 KB)
- Français - FR (604 KB)
- Deutsch - DE (604 KB)
- Norwegian - NO (604 KB)
- Español - ES (604 KB)
- Swedish - SV (604 KB)
- Italian - IT (604 KB)
- Korean - KR (604 KB)
- Portuguese - PT (604 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Garofalo AW, et al. Selective Inhibitors of G2019S-LRRK2 Kinase Activity. J Med Chem. 2020 Dec 10;63(23):14821-14839. [Content Brief]
[2]. Thakur G, et al. Structural Insights and Development of LRRK2 Inhibitors for Parkinson's Disease in the Last Decade. Genes (Basel). 2022 Aug 11;13(8):1426. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4128 mL | 12.0639 mL | 24.1278 mL | 60.3195 mL |
| 5 mM | 0.4826 mL | 2.4128 mL | 4.8256 mL | 12.0639 mL | |
| 10 mM | 0.2413 mL | 1.2064 mL | 2.4128 mL | 6.0319 mL | |
| 15 mM | 0.1609 mL | 0.8043 mL | 1.6085 mL | 4.0213 mL | |
| 20 mM | 0.1206 mL | 0.6032 mL | 1.2064 mL | 3.0160 mL | |
| 25 mM | 0.0965 mL | 0.4826 mL | 0.9651 mL | 2.4128 mL | |
| 30 mM | 0.0804 mL | 0.4021 mL | 0.8043 mL | 2.0106 mL | |
| 40 mM | 0.0603 mL | 0.3016 mL | 0.6032 mL | 1.5080 mL | |
| 50 mM | 0.0483 mL | 0.2413 mL | 0.4826 mL | 1.2064 mL | |
| 60 mM | 0.0402 mL | 0.2011 mL | 0.4021 mL | 1.0053 mL | |
| 80 mM | 0.0302 mL | 0.1508 mL | 0.3016 mL | 0.7540 mL | |
| 100 mM | 0.0241 mL | 0.1206 mL | 0.2413 mL | 0.6032 mL |
EB-42486 Related Classifications
HY-142647 Related Classifications
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