Linoleoyl Glycine
(Synonyms: Glycine Linoleamide, LinGly, NLinoleoyl Glycine) 目录号 : GC44074A homolog of arachidonyl glycine
Cas No.:2764-03-6
Sample solution is provided at 25 µL, 10mM.
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- Purity: >98.00%
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Arachidonyl glycine, the conjugate of arachidonic acid and glycine produced in mammalian brain, skin, and spinal cord, is a structural analog of anandamide (AEA) that is reported to have analgesic activities in whole animal experiments. It has poor affinity for the central cannabinoid (CB1) receptor, high-affinity for the G protein-coupled receptor GPR-18, and is metabolically regulated by fatty acid amide hydrolase (FAAH) activity. LinGly is an endogenous homolog of linoleoyl ethanolamide, an arachidonyl glycine. It inhibits the hydrolysis of AEA in FAAH-containing N18TG2 cell membranes with an IC50 value of ~25 µM, which is less potent than that of arachidonyl glycine (IC50 = 7 µM). The biological significance of LinGly has not yet been determined.
Cas No. | 2764-03-6 | SDF | |
别名 | Glycine Linoleamide, LinGly, NLinoleoyl Glycine | ||
Canonical SMILES | CCCCC/C=C\C/C=C\CCCCCCCC(=O)NCC(=O)O | ||
分子式 | C20H35NO3 | 分子量 | 337.5 |
溶解度 | DMF: 20 mg/ml,DMSO: 15 mg/ml,Ethanol: 25 mg/ml,PBS (pH 7.2): 2 mg/ml | 储存条件 | Store at -20°C |
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制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.963 mL | 14.8148 mL | 29.6296 mL |
5 mM | 0.5926 mL | 2.963 mL | 5.9259 mL |
10 mM | 0.2963 mL | 1.4815 mL | 2.963 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 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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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。
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Polyunsaturated fatty acid-derived IKs channel activators shorten the QT interval ex-vivo and in-vivo
Acta Physiol (Oxf) 2020 Aug;229(4):e13471.PMID:32223014DOI:10.1111/apha.13471.
Aim: We aimed to assess the ability of natural and modified polyunsaturated fatty acids (PUFAs) to shorten QT interval in ex-vivo and in-vivo guinea pig hearts. Methods: The effect of one natural (docosahexaenoic acid [DHA]) and three modified (Linoleoyl Glycine [Lin-GLY], docosahexaenoyl glycine [DHA-GLY], N-arachidonoyl taurine [N-AT]) PUFAs on ventricular action potential duration (APD) and QT interval was studied in a E4031 drug-induced long QT2 model of ex-vivo guinea pig hearts. The effect of DHA-GLY on QT interval was also studied in in-vivo guinea pig hearts upon intravenous administration. The effect of modified PUFAs on IKs was studied using Xenopus laevis oocytes expressing human KCNQ1 and KCNE1. Results: All tested PUFAs shortened ADP and QT interval in ex-vivo guinea pig hearts, however, with different ability in restoring baseline APD/QT interval with specific modified PUFAs being most efficacious. Despite comparable ability in activating the human KCNQ1/KCNE1 channel, Lin-GLY was not as effective in shortening APD/QT interval as DHA-GLY in ex-vivo hearts. By constructing a guinea pig-like KCNE1, we found Lin-GLY to induce less activating effect compared with DHA-GLY on human KCNQ1 co-expressed with guinea pig-like KCNE1. Docosahexaenoyl glycine was studied in more detail and was found to shorten QT interval in in-vivo guinea pig hearts. Conclusion: Our results show that specific PUFAs shorten QT interval in guinea pig hearts. The tendency of modified PUFAs with pronounced IKs channel activating effect to better restore QT interval suggests that modifying PUFAs to target the IKs channel is a means to improve the QT-shortening effect.