RN277
Based on 1 Customer Validation
RN277 is a selective LRRK2 inhibitor with an IC50 of 135 nM against LRRK2RCKW kinase. RN277 inhibits LRRK2-mediated phosphorylation of Rab8a. RN277 rescues the motor activity of kinesin inhibited by LRRK2RCKW in vitro, and its mechanism of action may involve preventing LRRK2 from forming filamentous structures on microtubules. RN277 can be used in studies related to Parkinson's disease.
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- Purity: 99.08%
- 화학식: C31H33ClN8O2
- 분자량:585.10
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보관: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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
RN277 (4 h) inhibits LRRK2RCKW-mediated phosphorylation of its physiological substrate Rab8a in vitro, with an IC50 of 70 nM[1].
RN277 (0.25-5 µM; 4 h) dose-dependently inhibits LRRK2-mediated Rab8a phosphorylation in 293T cells, reducing the phosphorylation level to near background at 5 µM, without affecting the S935 phosphorylation of LRRK2[1].
RN277 (5 µM; 10 min pre-incubation with LRRK2RCKW, 5 min incubation with microtubules) restores the microtubule motility of K560-GFP kinesin inhibited by LRRK2RCKW[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:293T cells co-transfected with full-length LRRK2 and GFP-Rab8a
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Concentration:0.25, 0.5, 1, 2.5, 5, 250, 500, 1, 2.5, 5 µM
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Incubation Time:4 h
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Result:Reduced Rab8a phosphorylation in a dose-dependent manner.
Reduced phosphorylated Rab8a to near background levels at 5 µM, comparable to the positive control MLi-2.
Did not significantly reduce phosphorylation of the LRRK2 biomarker site S935.
Chemical Information
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Appearance Solid
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분자량 585.10
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화학식 C31H33ClN8O2
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Color White to off-white
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SMILES
ClC1=NC(N2CCOCC2)=C(C(C3=CC=CC(NC(NC4=CC(C(C)(C)C)=NN4C5=CC=C(C)C=C5)=O)=C3)=CN6)C6=N1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 25 mg/mL (42.73 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: ≥ 2.5 mg/mL (4.27 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.27 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 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 (25.0 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.
순도&문서
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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 | 1.7091 mL | 8.5455 mL | 17.0911 mL | 42.7277 mL |
| 5 mM | 0.3418 mL | 1.7091 mL | 3.4182 mL | 8.5455 mL | |
| 10 mM | 0.1709 mL | 0.8546 mL | 1.7091 mL | 4.2728 mL | |
| 15 mM | 0.1139 mL | 0.5697 mL | 1.1394 mL | 2.8485 mL | |
| 20 mM | 0.0855 mL | 0.4273 mL | 0.8546 mL | 2.1364 mL | |
| 25 mM | 0.0684 mL | 0.3418 mL | 0.6836 mL | 1.7091 mL | |
| 30 mM | 0.0570 mL | 0.2849 mL | 0.5697 mL | 1.4243 mL | |
| 40 mM | 0.0427 mL | 0.2136 mL | 0.4273 mL | 1.0682 mL |
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