JH-II-127
Based on 1 Customer Validation
JH-II-127 is an orally active, highly potent, selective and brain-permeable LRRK2 inhibitor, with IC50s of 6, 2 and 48 nM for wild-type LRRK2 and LRRK2-G2019S and mutant LRRK2-A2016T. JH-II-127 inhibits Ser935 phosphorylation in all tissues of mice, including the brain. JH-II-127 can be used in the study of parkinson's syndrome.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.0%
- No. CAS: 1700693-08-8
- Fòrmula: C19H21ClN6O3
- Peso molecular:416.86
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Almacenamiento: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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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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Orally Active Compound Library
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Anti-Parkinson's Disease Compound Library
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Neurodegenerative Disease-related Compound Library
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Heterocyclic Compound Library
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Highly Selective Inhibitors Library
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Serine/Threonine Kinase Inhibitor Library
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Autophagy Compound Library
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Actividad biológica
JH-II-127 (0.03, 0.1, 0.3, 1, 3 µM; 90 min) inhibits LRRK2 in HEK293 cells[1].
JH-II-127 (0.3, 1, 3 µM; 90 min) inhibits endogenously expressed LRRK2 in mouse Swiss 3T3 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells (expressing GFP-LRRK2, GFP-LRRK2[G2019S], GFP-LRRK2[G2019S + A2016T], and GFP-LRRK2[A2016T], respectively)
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Concentration:0.03, 0.1, 0.3, 1, 3 µM
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Incubation Time:90 min
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Result:Induced a dose-dependent inhibition of Ser910 and Ser935 phosphorylation in both wild-type LRRK2 and LRRK2[G2019S] stably transfected into HEK293 cells.
Inhibited phosphorylation of Ser910 and Ser935 at approximately 0.3 μM for wild-type LRRK2 and LRRK2[G2019S].
Induced dephosphorylation of Ser910 and Ser935 at a concentration of 0.3-1 μM in the drug-resistant LRRK2[A2016T + G2019S] and LRRK2[A2016T] mutants.
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Cell Line:Mouse Swiss 3T3 cells
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Concentration:0.03, 0.1, 0.3, 1, 3 µM
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Incubation Time:90 min
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Result:Induced similar dose-dependent Ser935 dephosphorylation of endogenous LRRK2.
| matrix | route | Tmax (h) | C0/Cmax (ng/mL) | AUCLast (h•ng/mL) | AUGINF (h•ng/mL) | T1/2 (h) | CL (mL/min/kg) | Vss (L/kg) |
| plasma | IV (2 mg/kg) | - | 1604.47 | 532.67 | 535.57 | 0.66 | 62.24 | 1.73 |
| plasma | PO (10 mg/kg) | 1 | 802.72 | 3094.58 | 3867.07 | - | - | - |
| brain | IV (2 mg/kg) | - | 1343.6 | 239.31 | 246.47 | 0.23 | 135.24 | 1.7 |
| brain | PO (10 mg/kg) | 1 | 247.35 | 688.21 | 762.38 | - | - | - |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wild type male C57BL/6 mice[1].
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Dosage:2 mg/kg (for i.v.); 10 mg/kg (for p.o.); 10, 30, 100 mg/kg (for i.p.)
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Administration:Intravenous and intraperitoneal injection; oral administration; single.
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Result:Led to near complete dephosphorylation of Ser935 of LRRK2 in all tissues including brain when at 100 mg/kg of i.p. and near complete inhibition in all tissues at 30 mg/kg but only partial inhibition in brain at the 10 mg/kg dose.
Demonstrated good oral bioavailability.
Chemical Information
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No. CAS 1700693-08-8
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Appearance Solid
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Peso molecular 416.86
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Fòrmula C19H21ClN6O3
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Color Light yellow to yellow
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SMILES
O=C(C1=CC=C(NC2=NC3=NC=C(Cl)C3=C(NC)N2)C(OC)=C1)N4CCOCC4
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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 2 years -20°C 1 year
Solvente y solubilidad
DMSO : 110 mg/mL (263.88 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.
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: ≥ 2.75 mg/mL (6.60 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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, 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 | 2.3989 mL | 11.9944 mL | 23.9889 mL | 59.9722 mL |
| 5 mM | 0.4798 mL | 2.3989 mL | 4.7978 mL | 11.9944 mL | |
| 10 mM | 0.2399 mL | 1.1994 mL | 2.3989 mL | 5.9972 mL | |
| 15 mM | 0.1599 mL | 0.7996 mL | 1.5993 mL | 3.9981 mL | |
| 20 mM | 0.1199 mL | 0.5997 mL | 1.1994 mL | 2.9986 mL | |
| 25 mM | 0.0960 mL | 0.4798 mL | 0.9596 mL | 2.3989 mL | |
| 30 mM | 0.0800 mL | 0.3998 mL | 0.7996 mL | 1.9991 mL | |
| 40 mM | 0.0600 mL | 0.2999 mL | 0.5997 mL | 1.4993 mL | |
| 50 mM | 0.0480 mL | 0.2399 mL | 0.4798 mL | 1.1994 mL | |
| 60 mM | 0.0400 mL | 0.1999 mL | 0.3998 mL | 0.9995 mL | |
| 80 mM | 0.0300 mL | 0.1499 mL | 0.2999 mL | 0.7497 mL | |
| 100 mM | 0.0240 mL | 0.1199 mL | 0.2399 mL | 0.5997 mL |
JH-II-127 Related Classifications
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