CAY10499 (MAGL-IN-5) (Synonyms: CAY10499) |
Catalog No.GC14244
One-Click Copy Product Info
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CAY10499 is a non-selective lipase inhibitor with IC50 values of 144, 90, and 14 nM for human recombinant monoacylglycerol lipase(MAGL),hormone sensitive lipase(HSL), and fatty acid amide hydrolase(FAAH) respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 359714-55-9
Sample solution is provided at 25 µL, 10mM.
CAY10499 (MAGL-IN-5) is a non-selective lipase inhibitor with IC50 values of 144nM and 14nM for monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH), respectively[1]. CAY10499 can reduce viral replication and pro-inflammatory cytokine levels by inhibiting lipolysis[2]. CAY10499 has been widely used to inhibit the activity of hormone-sensitive lipase (HSL) and to reduce StAR protein expression and progesterone synthesis[3].
In vitro, CAY10499 treatment for 96 hours significantly inhibited the proliferation of OVCAR3, COV318, and CAOV3 cells, with IC50 values of 43μM, 59μM, and 77μM, respectively[4]. The 1-hour pretreatment with 20μM CAY10499 significantly reduced the mRNA expression of IL-6 and IL-8 in adipocytes induced by lipopolysaccharide (LPS)[5]. Treatment with 10μM CAY10499 in combination with N-palmitoylethanolamine (PEA) for 72 hours significantly induced cell death in B16 cells[6].
In vivo, intraperitoneal injection of CAY10499 at 10mg/kg (twice a day) for 4 days significantly increased the survival rate of mice infected with influenza A virus (IAV)[7].
References:
[1] Granchi C, Rizzolio F, Bordoni V, et al. 4-Aryliden-2-methyloxazol-5 (4 H)-one as a new scaffold for selective reversible MAGL inhibitors[J]. Journal of Enzyme Inhibition and Medicinal Chemistry, 2016, 31(1): 137-146.
[2] Cesar-Silva D, Pereira-Dutra F S, Giannini A L M, et al. Lipid compartments and lipid metabolism as therapeutic targets against coronavirus[J]. Frontiers in Immunology, 2023, 14: 1268854.
[3] Manna P R, Cohen-Tannoudji J, Counis R, et al. Mechanisms of action of hormone-sensitive lipase in mouse Leydig cells: its role in the regulation of the steroidogenic acute regulatory protein[J]. Journal of Biological Chemistry, 2013, 288(12): 8505-8518.
[4] Aghazadeh Tabrizi M, Baraldi P G, Baraldi S, et al. Discovery of 1, 5-diphenylpyrazole-3-carboxamide derivatives as potent, reversible, and selective monoacylglycerol lipase (MAGL) inhibitors[J]. Journal of medicinal chemistry, 2018, 61(3): 1340-1354.
[5] Aghazadeh Tabrizi M, Baraldi P G, Baraldi S, et al. Discovery of 1, 5-diphenylpyrazole-3-carboxamide derivatives as potent, reversible, and selective monoacylglycerol lipase (MAGL) inhibitors[J]. Journal of medicinal chemistry, 2018, 61(3): 1340-1354.
[6] Hamtiaux L, Masquelier J, Muccioli G G, et al. The association of N-palmitoylethanolamine with the FAAH inhibitor URB597 impairs melanoma growth through a supra-additive action[J]. BMC cancer, 2012, 12(1): 92.
[7] Baek Y B, Kwon H J, Sharif M, et al. Therapeutic strategy targeting host lipolysis limits infection by SARS-CoV-2 and influenza A virus[J]. Signal Transduction and Targeted Therapy, 2022, 7(1): 367.
| Cell experiment [1]: | |
Cell lines | OVCAR3 cells |
Preparation Method | OVCAR3 cells were grown in DMEM medium supplemented with 10% fetal bovine serum and 1% penicillin/streptomycin in 5% CO2 at 37°C. Cells (5×103 cells/ml) were seeded in 96-well plates and allowed to adhere in a 5% CO2 incubator at 37°C overnight, and were treated with different concentrations of CAY10499 (0.01, 0.1, 1, 10, and 100μM) for 96h. The cell viability was evaluated. |
Reaction Conditions | 0.01, 0.1, 1, 10, and 100μM; 96h |
Applications | CAY10499 treatment significantly reduced the cell viability of OVCAR3 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female C57BL/6J mice |
Preparation Method | Female C57BL/6J mice (seven weeks old; 22-25g) were kept under standard conditions (temperature 22±2°C and humidity 50%-60% on a 12h light/dark cycle) with free to food and water ad libitum. After 1 week of acclimatization, the mice were infected with the IAV virus and then received intraperitoneal injections of 10mg/kg dose of CAY10499 twice a day for 4 days. Then, the survival of the mice within 10 days was analyzed. |
Dosage form | 10mg/kg; twice a day; 4 days; p.o. |
Applications | CAY10499 treatment significantly enhanced the survival of the IAV-challenged mice. |
References: | |
| Cas No. | 359714-55-9 | SDF | |
| Synonyms | CAY10499 | ||
| Chemical Name | [4-(5-methoxy-2-oxo-1,3,4-oxadiazol-3(2H)-yl)-2-methylphenyl]-carbamic acid, phenylmethyl ester | ||
| Canonical SMILES | CC1=CC(N(N=C(O2)OC)C2=O)=CC=C1NC(OCC3=CC=CC=C3)=O | ||
| Formula | C18H17N3O5 | M.Wt | 355.3 |
| Solubility | 20mg/mL in DMSO, 20mg/mL in DMF, 2mg/mL in Ethanol | Storage | Store at -20°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8145 mL | 14.0726 mL | 28.1452 mL |
| 5 mM | 562.9 μL | 2.8145 mL | 5.629 mL |
| 10 mM | 281.5 μL | 1.4073 mL | 2.8145 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)