Eicosapentaenoyl Serotonin
目录号 : GC12772
A potential TRPV1 antagonist
Cas No.:199875-71-3
Sample solution is provided at 25 µL, 10mM.
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Eicosapentaenoyl serotonin is a hybrid molecule patterned after arachidonoyl serotonin. Arachidonoyl serotonin is an inhibitor of fatty acid amide hydrolase (FAAH) and also acts as an antagonist of transient receptor potential vanilloid-type 1 (TRPV1) channels. Arachidonoyl serotonin is analgesic, reducing both acute and chronic peripheral pain in rodents [1, 2]. The effects of replacement the arachidonoyl portion with eicosapentaenoic acid have not been investigated. Replacement of arachidonate with saturated 11- or 12-carbon fatty acids generated compounds that potently inhibited capsaicin-induced TRPV1 channel activation with an IC50 of 0.76 μM. This compound showed no effects on blocking FAAH-mediated hydrolysis of arachidonoyl ethanolamide with an IC50 of > 50 μM [1].
References:
[1] Ortar, G. ,Cascio, M.G.,De Petrocellis, L., et al. New N-arachidonoylserotonin analogues with potential "dual" mechanism of action against pain. Journal of Medicinal Chemistry 50, 6554-6569 (2007).
[2] Maione, S. ,De Petrocellis, L.,de Novellis, V., et al. Analgesic actions of N-arachidonoyl-serotonin, a fatty acid amide hydrolase inhibitor with antagonistic activity at vanilloid TRPV1 receptors. British Journal of Pharmacology 150, 766-781 (2007).
| Cas No. | 199875-71-3 | SDF | |
| 化学名 | N-[2-(5-hydroxy-1H-indol-3-yl)ethyl]-5Z,8Z,11Z,14Z,17Z-eicosapentaenamide | ||
| Canonical SMILES | O=C(NCCC1=CNC2=CC=C(O)C=C12)CCC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CC | ||
| 分子式 | C30H40N2O2 | 分子量 | 460.7 |
| 溶解度 | ≤20mg/ml in ethanol;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 | 2.1706 mL | 10.853 mL | 21.7061 mL |
| 5 mM | 0.4341 mL | 2.1706 mL | 4.3412 mL |
| 10 mM | 0.2171 mL | 1.0853 mL | 2.1706 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