CAY10499 (Synonyms: CAY10499) |
| Catalog No.GC14244 |
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 is a potent inhibitor of monoglyceride lipase (MGL) [1] and human hormone sensitive lipase [2].
Monoglyceride lipase (MGL) plays an important role in the metabolism of the lipid transmitter 2-arachidonoylglycerol (2-AG). This endocannabinoid has been known to mediate various physiological processes, and its regulation is thought to be of great therapeutic potential[1]. Hormone sensitive lipase (HSL) has been involved in catalyzing the hydrolysis of tri-, di-, and monoacylglycerols, and cholesterol esters, thus mobilizing fatty acids as a primary source of energy in mammals. The HSL enzyme is highly expressed in adipose tissue and steroidogenic tissue and implicated in diverse physiology roles including those in steroidogenesis and spermatogenesis, foam cell formation in atherosclerosis, and diabetes [3].
CAY10499 inhibited MGL-mediated 4-NPA hydrolysis with the IC 50 value of 0.5 ± 0.03 μM. CAY10499 fully inhibited [3H]-AEA hydrolysis by human recombinant FAAH with an IC50 of 76 nM. CAY10499 displaced only 25% and 20% of [3H]-CP-55940-specific binding to the CB1 and CB2 receptors, respectively [1]. CAY10499 potently inhibited the activity of human hormone sensitive lipase with an IC50 of 90 nM for the recombinant human hormone sensitive lipase enzyme [2].
References:
[1] Muccioli G G, Labar G, Lambert D M. CAY10499, a novel monoglyceride lipase inhibitor evidenced by an expeditious MGL assay[J]. ChemBioChem, 2008, 9(16): 2704-2710.
[2] Ben Ali Y, Muller G, Petry S, et al. Kinetic characterization and specific inhibition of hormone sensitive lipase[C]//CHEMISTRY AND PHYSICS OF LIPIDS. ELSEVIER HOUSE, BROOKVALE PLAZA, EAST PARK SHANNON, CO, CLARE, 00000, IRELAND: ELSEVIER IRELAND LTD, 2005, 136(2): 155-155.
[3] Kraemer F B, Shen W J. Hormone-sensitive lipase control of intracellular tri-(di-) acylglycerol and cholesteryl ester hydrolysis[J]. Journal of lipid research, 2002, 43(10): 1585-1594.
| 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 | 0.5629 mL | 2.8145 mL | 5.629 mL |
| 10 mM | 0.2815 mL | 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 ddH2O, 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.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)
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