| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
Monoacylglycerol lipase (MAGL)
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|---|---|
| ln Vitro |
The compound acts as a selective and reversible MAGL inhibitor. By inhibiting MAGL, it prevents the hydrolysis of the endocannabinoid 2-arachidonoylglycerol (2-AG) to arachidonic acid and glycerol, thereby elevating 2-AG levels and reducing pro-inflammatory prostaglandin production.
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| ln Vivo |
No standardized in vivo data is publicly available. MAGL inhibitors are known to produce analgesic, anti-inflammatory, and anti-tumor effects in animal models. This compound is designed for studying inflammation, cancer, and oxidative stress pathways in experimental systems.
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| Enzyme Assay |
Recombinant human MAGL is incubated with a fluorogenic substrate (e.g., arachidonoyl-7-hydroxy-6-methoxy-4-methylcoumarin ester) in assay buffer. Test compound is added at varying concentrations, and fluorescence increase due to hydrolysis is monitored. IC50 values are calculated from inhibition curves.
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| Cell Assay |
Cell-based studies typically involve treating cancer cells (e.g., HEK293, PC3) or macrophages with the compound for 24-72 hours. Intracellular 2-AG levels are measured by LC-MS, and downstream signaling markers including prostaglandins and inflammatory cytokines are quantified.
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| Animal Protocol |
No specific in vivo protocol is documented. Standard animal models include carrageenan-induced paw edema for anti-inflammatory studies and xenograft tumor models for cancer research. Efficacy is assessed by measuring inflammatory markers and tumor growth inhibition.
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| ADME/Pharmacokinetics |
MAGL-IN-11 is described as having very good ADME properties and low in vivo toxicity. Detailed PK parameters including half-life, clearance, and oral bioavailability are not specified in standard databases but are favorable for in vivo use.
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| Toxicity/Toxicokinetics |
The compound is described as having low in vivo toxicity, a key feature distinguishing it from other MAGL inhibitors. No specific toxicological data is available, but the favorable toxicity profile suggests suitability for prolonged in vivo pharmacology studies.
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| References | |
| Additional Infomation |
This compound is a MAGL inhibitor for research use in inflammation, cancer, and antioxidant studies. It is not approved for human use and is strictly an investigational chemical tool for probing the endocannabinoid system.
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| Molecular Formula |
C24H21F4N3O2S
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|---|---|
| Molecular Weight |
491.5
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| CAS # |
3017151-84-4
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| Appearance |
Typically exists as solid at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0346 mL | 10.1729 mL | 20.3459 mL | |
| 5 mM | 0.4069 mL | 2.0346 mL | 4.0692 mL | |
| 10 mM | 0.2035 mL | 1.0173 mL | 2.0346 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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