MAGL-IN-1
Based on 1 publication(s) in Google Scholar
MAGL-IN-1 is a potent, selective, reversible and competitive inhibitor of MAGL, with an IC50 of 80 nM. MAGL-IN-1 exhibits anti-proliferative effects against human breast, colorectal, and ovarian cancer cells. MAGL-IN-1 blocks MAGL in cell-based as well as in vivo assays.
For research use only. We do not sell to patients.
- Purity: 99.45%
- CAS No.: 2324160-91-8
- Formula: C22H24FNO3
- Molecular Weight:369.43
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) MAGL-IN-1
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Biological Activity
IC50: 80 nM (MAGL)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Caov-3 cell line | IC50 |
25 μM
Compound: 23
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Growth inhibition of human Caov3 cells after 96 hrs by celltiter-glo assay
Growth inhibition of human Caov3 cells after 96 hrs by celltiter-glo assay
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[PMID: 30715876] |
| HCT-116 | IC50 |
21 μM
Compound: 23
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Growth inhibition of human HCT116 cells after 96 hrs by celltiter-glo assay
Growth inhibition of human HCT116 cells after 96 hrs by celltiter-glo assay
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[PMID: 30715876] |
| HEK293 | IC50 |
>10 μM
Compound: 23
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Inhibition of human ABHD12 expressed in HEK293 cell homogenates pre-incubated for 30 mins in presence of [1,2,3-3H]2-OG by liquid scintillation spectroscopy
Inhibition of human ABHD12 expressed in HEK293 cell homogenates pre-incubated for 30 mins in presence of [1,2,3-3H]2-OG by liquid scintillation spectroscopy
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[PMID: 30715876] |
| HEK293 | IC50 |
>10 μM
Compound: 23
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Inhibition of human ABHD6 expressed in HEK293 cell homogenates pre-incubated for 30 mins in presence of [1,2,3-3H]2-OG by liquid scintillation spectroscopy
Inhibition of human ABHD6 expressed in HEK293 cell homogenates pre-incubated for 30 mins in presence of [1,2,3-3H]2-OG by liquid scintillation spectroscopy
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[PMID: 30715876] |
| MDA-MB-231 | IC50 |
7.9 μM
Compound: 23
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Growth inhibition of human MDA-MB-231 cells after 96 hrs by celltiter-glo assay
Growth inhibition of human MDA-MB-231 cells after 96 hrs by celltiter-glo assay
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[PMID: 30715876] |
| MRC5 | IC50 |
>100 μM
Compound: 23
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Growth inhibition of human MRC5 cells after 96 hrs by celltiter-glo assay
Growth inhibition of human MRC5 cells after 96 hrs by celltiter-glo assay
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[PMID: 30715876] |
| OVCAR-3 | IC50 |
57 μM
Compound: 23
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Growth inhibition of human OVCAR3 cells after 96 hrs by celltiter-glo assay
Growth inhibition of human OVCAR3 cells after 96 hrs by celltiter-glo assay
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[PMID: 30715876] |
| SK-OV-3 | IC50 |
15 μM
Compound: 23
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Growth inhibition of human SKOV3 cells after 96 hrs by celltiter-glo assay
Growth inhibition of human SKOV3 cells after 96 hrs by celltiter-glo assay
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[PMID: 30715876] |
MAGL-IN-1 (compound 23) (0.02-200 μM; 96 h) produces an appreciable inhibition of cell viability in all the tested cancer cell lines, with IC50s ranging from 7.9 to 57 μM[1].
MAGL-IN-1 (0.125-1 μM; 30 min) competitively binds to MAGL with 4-nitrophenylacetate, with a Ki of 39 nM[1].
MAGL-IN-1 (10 μM; 90 min) does not significantly inhibit CB1, CB2, FAAH, ABHD6 and ABHD12 activity at the concentration of 10 μM[1].
MAGL-IN-1 (1 nM-100 μM; 15 min) inhibits [3H]2-oleoyl glycerol (2-OG) hydrolysis in a concentration dependent manner in U937 cells, with an IC50 of 193 nM[1].
MAGL-IN-1 (0.01-30 μM; 15 min) inhibits 2-OG hydrolysis in a concentration-dependent manner in mouse brain membrane preparations, with an IC50 of 2.1 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116, MDA-MB-231, CAOV3, OVCAR3, SKOV3, and MRC5 cells
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Concentration:0.02-200 μM
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Incubation Time:96 hours
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Result:Inhibited the growth of human breast MDA-MB-231, colorectal HCT116, and ovarian CAOV3, OVCAR3, and SKOV3 cancer cells, with IC50s of 7.9, 21, 25, 57, and 15 μM, respectively.
Was inactive against MRC5 (IC50>100 μM).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL6 mice, 8-10 weeks old[1]
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Dosage:50 mg/kg
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Administration:Intraperitoneal injection; once
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Result:Increased 2-AG levels in the brain and plasma.
Chemical Information
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CAS No. 2324160-91-8
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Appearance Solid
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Molecular Weight 369.43
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Formula C22H24FNO3
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Color White to off-white
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SMILES
O=C(C1CCN(C(C2=CC(O)=CC=C2F)=O)CC1)C3=CC=C(C(C)C)C=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
DMSO : 62.5 mg/mL (169.18 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 (5.63 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 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 (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 (5.63 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.
Purity & Documentation
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Data Sheet (272 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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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 | 2.7069 mL | 13.5344 mL | 27.0687 mL | 67.6718 mL |
| 5 mM | 0.5414 mL | 2.7069 mL | 5.4137 mL | 13.5344 mL | |
| 10 mM | 0.2707 mL | 1.3534 mL | 2.7069 mL | 6.7672 mL | |
| 15 mM | 0.1805 mL | 0.9023 mL | 1.8046 mL | 4.5115 mL | |
| 20 mM | 0.1353 mL | 0.6767 mL | 1.3534 mL | 3.3836 mL | |
| 25 mM | 0.1083 mL | 0.5414 mL | 1.0827 mL | 2.7069 mL | |
| 30 mM | 0.0902 mL | 0.4511 mL | 0.9023 mL | 2.2557 mL | |
| 40 mM | 0.0677 mL | 0.3384 mL | 0.6767 mL | 1.6918 mL | |
| 50 mM | 0.0541 mL | 0.2707 mL | 0.5414 mL | 1.3534 mL | |
| 60 mM | 0.0451 mL | 0.2256 mL | 0.4511 mL | 1.1279 mL | |
| 80 mM | 0.0338 mL | 0.1692 mL | 0.3384 mL | 0.8459 mL | |
| 100 mM | 0.0271 mL | 0.1353 mL | 0.2707 mL | 0.6767 mL |