Arachidonic Acid Leelamide
目录号 : GC16770
A novel fatty acid amide
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 | ||
| 化学名 | 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 | ||
| 分子式 | C40H61NO | 分子量 | 571.9 |
| 溶解度 | ≤20mg/ml in DMSO;20mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7486 mL | 8.7428 mL | 17.4856 mL |
| 5 mM | 0.3497 mL | 1.7486 mL | 3.4971 mL |
| 10 mM | 0.1749 mL | 0.8743 mL | 1.7486 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet