GNE-9605
Based on 1 Customer Validation
GNE-9605 is a potent, orally active, selective Leucine-rich repeat kinase 2 (LRRK2) inhibitor with an IC50 value of 18.7 nM. GNE-9605 inhibits LRRK2 Ser1292 autophosphorylation. GNE-9605 can be used in research of Parkinson's disease (PD) .
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.51%
- CAS 番号: 1536200-31-3
- 分子式: C17H20ClF4N7O
- 分子量:449.83
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保管条件: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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Bioactive Compound Library Max
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Protein Kinase Compound Library
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Posttranslational Modification Library
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生物活性
GNE-9605 (1 mg/kg, p.o.; 0.5 mg/kg, i.v.; once) displays LRRK2 Ki in the biochemical assay of 2 nM as well as a cellular IC50 of 19 nM. GNE-9605 has a total plasma clearance with excellent oral bioavailability[1].
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[1].
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Dosage:10 and 50 mg/kg
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Administration:Intraperitoneal injection; once
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Result:Inhibited LRRK2 Ser1292 autophosphorylation in a dose-dependent manner.
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Animal Model:BAC transgenic mice expressing human LRRK2 protein[1].
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Dosage:1 mg/kg, p.o.; 0.5 mg/kg, i.v.
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Administration:Oral administration and intravenous injection; once
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Result:Demonstrated a total plasma clearance of 26 mL min-1 kg-1 with excellent oral bioavailability (90%).
化学情報
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CAS 番号 1536200-31-3
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性状 Solid
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分子量 449.83
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分子式 C17H20ClF4N7O
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Color White to off-white
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SMILES
FC(C1=CN=C(NC2=C(Cl)N([C@@H]3[C@@H](F)CN(C4COC4)CC3)N=C2)N=C1NC)(F)F
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
溶剤 & 溶解度
DMSO : 100 mg/mL (222.31 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, 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 (4.62 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 (4.62 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.
純度とドキュメンテーション
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データシート (273 KB)
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SDS (396 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Estrada AA, et, al. Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. J Med Chem. 2014 Feb 13;57(3):921-36. [Content Brief]
[2]. Kumar S, et, al. Exploring the focal role of LRRK2 kinase in Parkinson's disease. Environ Sci Pollut Res Int. 2022 May;29(22):32368-32382. [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, 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 | 2.2231 mL | 11.1153 mL | 22.2306 mL | 55.5766 mL |
| 5 mM | 0.4446 mL | 2.2231 mL | 4.4461 mL | 11.1153 mL | |
| 10 mM | 0.2223 mL | 1.1115 mL | 2.2231 mL | 5.5577 mL | |
| 15 mM | 0.1482 mL | 0.7410 mL | 1.4820 mL | 3.7051 mL | |
| 20 mM | 0.1112 mL | 0.5558 mL | 1.1115 mL | 2.7788 mL | |
| 25 mM | 0.0889 mL | 0.4446 mL | 0.8892 mL | 2.2231 mL | |
| 30 mM | 0.0741 mL | 0.3705 mL | 0.7410 mL | 1.8526 mL | |
| 40 mM | 0.0556 mL | 0.2779 mL | 0.5558 mL | 1.3894 mL | |
| 50 mM | 0.0445 mL | 0.2223 mL | 0.4446 mL | 1.1115 mL | |
| 60 mM | 0.0371 mL | 0.1853 mL | 0.3705 mL | 0.9263 mL | |
| 80 mM | 0.0278 mL | 0.1389 mL | 0.2779 mL | 0.6947 mL | |
| 100 mM | 0.0222 mL | 0.1112 mL | 0.2223 mL | 0.5558 mL |
GNE-9605 関連分類
HY-12282 関連分類
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