| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
CAY10499 targets monoglyceride lipase (MGL), fatty acid amide hydrolase (FAAH), and hormone sensitive lipase (HSL). MGL and FAAH are key enzymes in the metabolism of the endocannabinoid 2-arachidonoylglycerol (2-AG) and anandamide (AEA), respectively. HSL is involved in the hydrolysis of triglycerides and cholesterol esters, playing a crucial role in energy mobilization. By inhibiting these enzymes, CAY10499 modulates lipid signaling pathways.
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| ln Vitro |
In vitro, CAY10499 is a potent inhibitor of MGL, FAAH, and HSL. It inhibits MGL-mediated 4-NPA hydrolysis with an IC50 of 0.5 μM and fully inhibits FAAH-mediated [3H]-AEA hydrolysis with an IC50 of 76 nM. It also potently inhibits human HSL with an IC50 of 90 nM. The compound shows only weak binding to cannabinoid CB1 and CB2 receptors, displacing only 25% and 20% of specific binding, respectively, indicating its specificity is primarily towards the lipases rather than the cannabinoid receptors.
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| ln Vivo |
In vivo, CAY10499 is used to study the physiological roles of MGL, FAAH, and HSL. By inhibiting these enzymes, it can increase the levels of their respective substrates (e.g., 2-AG, AEA), which can have various effects on pain, inflammation, energy balance, and other physiological processes. Its use in animal models helps to elucidate the therapeutic potential of modulating the endocannabinoid system and lipid metabolism.
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| Enzyme Assay |
The in vitro activity of CAY10499 can be assessed using enzyme activity assays. For MGL activity, the enzyme is incubated with the substrate 4-nitrophenyl acetate (4-NPA) in the presence or absence of CAY10499. The hydrolysis of 4-NPA releases 4-nitrophenol, which can be measured spectrophotometrically at 405 nm. The IC50 is determined by plotting the enzyme activity against the logarithm of the inhibitor concentration. For FAAH, a similar approach using a radiolabeled substrate like [3H]-anandamide ([3H]-AEA) is employed.
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| Cell Assay |
Cellular assays are not the primary focus for CAY10499, as its activity is typically measured in cell-free enzyme assays. However, its effects can be studied in cell-based systems by measuring the levels of endocannabinoids (e.g., 2-AG, AEA) in cells treated with the compound. Cells are treated with CAY10499, and the levels of these lipids are then quantified using liquid chromatography-mass spectrometry (LC-MS). This demonstrates the compound's ability to inhibit the enzymes in a cellular context and modulate endocannabinoid levels.
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| Animal Protocol |
The in vivo activity of CAY10499 can be studied in animal models of pain, inflammation, or metabolic disorders. In these studies, the compound is typically administered via intraperitoneal or oral routes. The dosage and treatment regimen are optimized based on the specific model. The effects are then assessed by measuring behavioral responses (e.g., pain threshold), biochemical markers (e.g., endocannabinoid levels in the brain), or physiological parameters.
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| ADME/Pharmacokinetics |
Dosing is typically by intraperitoneal or oral administration. For pharmacokinetic studies, the compound is formulated in a suitable vehicle (e.g., DMSO, PEG400, or Tween 80) and administered to rodents. Blood and tissue samples are collected at various time points, and the concentration of CAY10499 is measured by LC-MS. These studies provide information on its absorption, distribution, metabolism, and excretion. Its molecular weight is 355.3.
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| Toxicity/Toxicokinetics |
The toxicity profile of CAY10499 is not extensively documented in the provided sources. As a research tool, it is handled with standard laboratory safety precautions. Its potential toxicity would be a consideration for in vivo studies, and appropriate dose ranges would be determined based on preliminary studies to avoid adverse effects while achieving the desired pharmacological effect.
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| References | |
| Additional Infomation |
CAY10499 is a carbamate.
CAY10499 is a research compound used as a potent inhibitor of multiple lipases, including MGL, FAAH, and HSL. It is a valuable tool for studying the endocannabinoid system and lipid metabolism. It is also known as MAGL-IN-5. It is not a therapeutic drug but is used in preclinical research to investigate the physiological and pathological roles of its target enzymes. |
| Molecular Formula |
C18H17N3O5
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|---|---|
| Molecular Weight |
355.35
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| Exact Mass |
355.116
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| CAS # |
359714-55-9
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| PubChem CID |
9924775
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.610
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| LogP |
1.97
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
26
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| Complexity |
547
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C=CC(=C1)N2C(=O)OC(=N2)OC)NC(=O)OCC3=CC=CC=C3
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| InChi Key |
QTENHWTVRQKWRI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H17N3O5/c1-12-10-14(21-18(23)26-17(20-21)24-2)8-9-15(12)19-16(22)25-11-13-6-4-3-5-7-13/h3-10H,11H2,1-2H3,(H,19,22)
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| Chemical Name |
benzyl N-[4-(5-methoxy-2-oxo-1,3,4-oxadiazol-3-yl)-2-methylphenyl]carbamate
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| Synonyms |
CAY 10499; CAY-10499; CAY10499
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO : ~100 mg/mL (~281.42 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.04 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.04 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8141 mL | 14.0706 mL | 28.1413 mL | |
| 5 mM | 0.5628 mL | 2.8141 mL | 5.6283 mL | |
| 10 mM | 0.2814 mL | 1.4071 mL | 2.8141 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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