Arachidonic Acid Leelamide |
カタログ番号GC16770
One-Click Copy Product Info
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ホスホリパーゼA2阻害剤
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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Arachidonic acid leelamide is a phospholipase A2 inhibitor.
Phospholipase A is a hydrolase responsible for the release of arachidonic acid from the sn2 position of phospholipids. The released arachidonic acid is then converted to mediators of inflammation by the enzymes prostaglandin synthetase and 5lipoxygenase, respectively. The inhibition of phospholipase A leads to a decrease in the release of arachidonic acid and, consequently, the inflammatory mediators.
In vitro: Arachidonic acid leelamide is the arachidonic amide analog of leelamine with no published pharmacological properties. For leelamine, it was found that electron micrographs of leelamine-treated cancer cells had accumulation of autophagosomes, membrane whorls, and lipofuscin-like structures. In addition, leelamine-mediated killing was a caspase-independent event triggered by cholesterol accumulation in the early process [1].
In vivo: In a previous study, authors identified the inductive effect of leelamine on CYP2B at doses of 5, 10, or 20 mg/kg in male ICR mice for 1 or 3 days. It was found that in liver, the activity of CYP2B significantly increased 3.6-fold after leelamine treatment. Activities of benzyloxyresorufin O-dealkylase and pentoxyresorufin O-dealkylase significantly increased 6.3- and 5.3-fold, respectively, with a single treatment of 20 mg/kg leelamine. Moreover, immunoblot analyses showed that significantly and dose-dependently increased CYP2B10 protein levels in liver. However, PCR results demonstrated that there were no significant changes in the CAR and CYP2B mRNA levels after leelamine treatment [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Kuzu OF, Gowda R, Sharma A, Robertson GP. Leelamine mediates cancer cell death through inhibition of intracellular cholesterol transport. Mol Cancer Ther. 2014 Jul;13(7):1690-703.
[2] Sim J, Nam W, Lee D, Lee S, O H, Joo J, Liu KH, Han JY, Ki SH, Jeong TC, Lee T, Lee S. Selective induction of hepatic cytochrome P450 2B activity by leelamine in vivo, as a potent novel inducer. Arch Pharm Res. 2015;38(5):725-33.
| Cas No. | SDF | ||
| Chemical Name | 1R,2,3,4,4aS,9,10,10aR-octahydro-1,4a-dimethyl-7-(1-methylethyl)-1-phenanthrene-5Z,8Z,11Z,14Z-eicosatetraenamide | ||
| Canonical SMILES | CC(C)C(C=C1)=CC2=C1[C@]3(C)[C@](CC2)([H])[C@@](CN([H])C(CCC/C=C\C/C=C\C/C=C\C/C=C\CCCCC)=O)(C)CCC3 | ||
| Formula | C40H61NO | M.Wt | 571.9 |
| 溶解度 | ≤20mg/ml in DMSO;20mg/ml in dimethyl formamide | Storage | Store at -20°C |
| 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 | 1.7486 mL | 8.7428 mL | 17.4856 mL |
| 5 mM | 349.7 μL | 1.7486 mL | 3.4971 mL |
| 10 mM | 174.9 μL | 874.3 μL | 1.7486 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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 36 reference(s) in Google Scholar.)