MAGL-IN-4
Based on 1 Customer Validation
MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 6.2 nM. MAGL-IN-4 can penetrate the blood-brain barrier (BBB). MAGL-IN-4 enhances endocannabinoid signaling mostly by the increase in the level of 2-AG via selective MAGL inhibition in the brain.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.79%
- CAS. Nr.: 2135785-20-3
- Formel: C18H21ClN2O4
- Molecular Weight:364.82
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Speicherung: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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Metabolism/Protease Compound Library
HY-L012
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CNS-Penetrant Compound Library
HY-L028
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Orally Active Compound Library
HY-L061
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Anti-Cancer Metabolism Compound Library
HY-L083
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Lipid Metabolism Compound Library
HY-L091
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Heterocyclic Compound Library
HY-L138
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Metabolic Enzyme Compound Library
HY-L146
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Highly Selective Inhibitors Library
HY-L158
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Biologische Aktivität
MAGL-IN-4 (compound 4f) shows a high LLE (5.9), a logD of 2.3 for MAGL[1].
MAGL-IN-4 exhibits no inhibition toward the closely related serine hydrolases (FAAH and ABHD6; all IC50>10000 nM). MAGL-IN-4 has no significant binding potentials to cannabinoid receptors (CB1: 19% and CB2: 5% at 10 μM), and low hERG liability (14.4% inh. at 10 μM, manual patch clamp, without BSA)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 2135785-20-3
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Appearance Solid
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Molecular Weight 364.82
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Formel C18H21ClN2O4
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Color White to off-white
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SMILES
CC1=C(C=C(C=C1)COC2CN(C([C@H]3C[C@]4(COC(N4)=O)C3)=O)C2)Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (274.11 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (6.85 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 (6.85 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 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.
Reinheit & Dokumentation
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
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 | 2.7411 mL | 13.7054 mL | 27.4108 mL | 68.5269 mL |
| 5 mM | 0.5482 mL | 2.7411 mL | 5.4822 mL | 13.7054 mL | |
| 10 mM | 0.2741 mL | 1.3705 mL | 2.7411 mL | 6.8527 mL | |
| 15 mM | 0.1827 mL | 0.9137 mL | 1.8274 mL | 4.5685 mL | |
| 20 mM | 0.1371 mL | 0.6853 mL | 1.3705 mL | 3.4263 mL | |
| 25 mM | 0.1096 mL | 0.5482 mL | 1.0964 mL | 2.7411 mL | |
| 30 mM | 0.0914 mL | 0.4568 mL | 0.9137 mL | 2.2842 mL | |
| 40 mM | 0.0685 mL | 0.3426 mL | 0.6853 mL | 1.7132 mL | |
| 50 mM | 0.0548 mL | 0.2741 mL | 0.5482 mL | 1.3705 mL | |
| 60 mM | 0.0457 mL | 0.2284 mL | 0.4568 mL | 1.1421 mL | |
| 80 mM | 0.0343 mL | 0.1713 mL | 0.3426 mL | 0.8566 mL | |
| 100 mM | 0.0274 mL | 0.1371 mL | 0.2741 mL | 0.6853 mL |
MAGL-IN-4 Related Classifications
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