GNE0877
Based on 2 publication(s) in Google Scholar
GNE0877 is a highly selective, orally active and brain-penetrant LRRK2 inhibitor with an IC50 of 3 nM and a Ki of 0.7 nM. GNE0877 can be used for the research of neuroscience.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.81%
- No. CAS: 1374828-69-9
- Fòrmula: C14H16F3N7
- Peso molecular:339.32
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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
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GNE0877
More
Actividad biológica
IC50: 3 nM (LRRK2)[1]
GNE0877 (1 μM; 10-30 min) shows good cellular potency in human liver microsomes and hepatocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human liver microsomes and hepatocytes
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Concentration:1 μM
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Incubation Time:10, 20 and 30 min
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Result:Exibited low turnover and good vitro stability in human liver microsomes and hepatocytes with no glucuronidation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation[1]
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Dosage:10 and 50 mg/kg
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Administration:Intraperitoneal injection; 10 and 50 mg/kg once
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Result:Tration-dependently inhibited Ser1292 autophosphorylation with an IC50 of 3 nM.
Chemical Information
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No. CAS 1374828-69-9
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Appearance Solid
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Peso molecular 339.32
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Fòrmula C14H16F3N7
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Color White to yellow
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SMILES
CC1=NN(C(C)(C)C#N)C=C1NC2=NC=C(C(F)(F)F)C(NC)=N2
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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
Publications (2)
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Journal Impact Factor
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Most Recent
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Hum Mol Genet
2017 Jul 15;26(14):2747-2767. PMID: 28453723 -
Solvente y solubilidad
DMSO : 250 mg/mL (736.77 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)
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 (6.13 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 (6.13 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 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.
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 (283 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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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.9471 mL | 14.7354 mL | 29.4707 mL | 73.6768 mL |
| 5 mM | 0.5894 mL | 2.9471 mL | 5.8941 mL | 14.7354 mL | |
| 10 mM | 0.2947 mL | 1.4735 mL | 2.9471 mL | 7.3677 mL | |
| 15 mM | 0.1965 mL | 0.9824 mL | 1.9647 mL | 4.9118 mL | |
| 20 mM | 0.1474 mL | 0.7368 mL | 1.4735 mL | 3.6838 mL | |
| 25 mM | 0.1179 mL | 0.5894 mL | 1.1788 mL | 2.9471 mL | |
| 30 mM | 0.0982 mL | 0.4912 mL | 0.9824 mL | 2.4559 mL | |
| 40 mM | 0.0737 mL | 0.3684 mL | 0.7368 mL | 1.8419 mL | |
| 50 mM | 0.0589 mL | 0.2947 mL | 0.5894 mL | 1.4735 mL | |
| 60 mM | 0.0491 mL | 0.2456 mL | 0.4912 mL | 1.2279 mL | |
| 80 mM | 0.0368 mL | 0.1842 mL | 0.3684 mL | 0.9210 mL | |
| 100 mM | 0.0295 mL | 0.1474 mL | 0.2947 mL | 0.7368 mL |
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