Eglumegad
Based on 4 publication(s) in Google Scholar
Eglumegad (LY354740) is a highly potent and selective group II (mGlu2/3) receptor agonist with IC50s of 5 nM and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.94%
- CAS 番号: 176199-48-7
- 分子式: C8H11NO4
- 分子量:185.18
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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MedChemExpress（MCE）の使用を引用している文献 Eglumegad
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生物活性
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mGluR2R 5 nM (IC50) |
mGluR3R 24 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Caco-2 | IC50 |
>10 mM
Compound: 1
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Inhibition of radiolabeled glycylsarcosine (Gly-Sar) uptake into Caco-2 cells done for 15 min at 37 degree C with compound
Inhibition of radiolabeled glycylsarcosine (Gly-Sar) uptake into Caco-2 cells done for 15 min at 37 degree C with compound
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[PMID: 16078848] |
| CHO | EC50 |
18.3 nM
Compound: 4, LY-354740
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Agonist activity against Metabotropic glutamate receptor 2 expressed in CHO cells was evaluated by measuring forskolin-induced cyclic AMP formation
Agonist activity against Metabotropic glutamate receptor 2 expressed in CHO cells was evaluated by measuring forskolin-induced cyclic AMP formation
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[PMID: 11123999] |
| HEK293 | EC50 |
>100 μM
Compound: 19
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Stimulation of [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells; Inactive
Stimulation of [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells; Inactive
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[PMID: 15801843] |
| HEK293 | IC50 |
458 μM
Compound: 17
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Inhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cells.
Inhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cells.
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[PMID: 10229625] |
Eglumegad (LY354740) down-regulates spots 1014, 1822 (hypoxia up-regulated protein 1), 4513 (an isoform of protein disulfide isomerase 3), 6204, 6312, 7306 (26S proteasome non-ATPase regulatory subunit 7) and protein spots 1013 and 6005 (destrin), and up-regulates spot 6507 (collapsin response mediator protein 1) in mouse cortical neurons[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 176199-48-7
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性状 Solid
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分子量 185.18
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分子式 C8H11NO4
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Color White to off-white
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SMILES
OC([C@]1([C@]2([H])[C@@H](C(O)=O)[C@]2([H])CC1)N)=O
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別名
LY354740; Eglumetad
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Cell Res
2025 Mar;35(3):165-185. PMID: 39875551 -
Neurobiol Dis
Distinct anti-dyskinetic effects of amantadine and group II metabotropic glutamate receptor agonist LY354740 in a rodent model: An electrophysiological perspective. [Abstract]2020 Jun;139:104807. PMID: 32088382 -
Front Pharmacol
LY354740 Reduces Extracellular Glutamate Concentration, Inhibits Phosphorylation of Fyn/NMDARs, and Expression of PLK2/pS129 α-Synuclein in Mice Treated With Acute or Sub-Acute MPTP. [Abstract]2020 Feb 28;11:183. PMID: 32180729 -
Pharmacol Biochem Behav
Activation of mGlu2/3 receptors in the striatum alleviates L-DOPA-induced dyskinesia and inhibits abnormal postsynaptic molecular expression. [Abstract]2023 Oct:231:173637. PMID: 37714223
溶剤 & 溶解度
H2O : 6.33 mg/mL (34.18 mM; Need ultrasonic and warming)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 2.86 mg/mL (15.44 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
プロトコル
Mice[1]
In Experiment 1A wild-type (female: N=6; male: N=5) and Gria1−/− mice (female: N=7; male: N=8) first receive 30 trials of drug-free testing (five trials per day for 6 days). Each animal is then tested on rewarded alternation following an injection of either Eglumegad (LY354740) (15 mg/kg) or vehicle. After injection animals are returned to the home cage for 30 min before behavioural testing commenced. Each animal is given 10 trials of rewarded alternation in the T-maze. Mice are given a maximum of 120 s to a complete a trial. At least 24 h after the first round of drug testing the animals are re-tested in the absence of any drug treatment to ensure that there are no long-term effects of the drug, and that the mice maintain a high level of alternation performance. Twenty-four hours after this re-testing, mice receive a further 10 trials of rewarded alternation testing, but now under the drug condition that they have not previously received. The order of drug exposure is counterbalanced within genotype and sex as far as possible given the numbers of mice. In all stages, the number of trials in which the animal alternated, as well as time taken to run from the start arm to the food well on the sample run (sample latency), and the time taken to run from the start arm to making a choice on the choice run (choice latency), are recorded. Latencies are measured by the experimenter using a stopwatch. The experimenter is blind to the genotype and drug allocations of the animals throughout testing. In Experiment 1B, separate groups of male wild-type (N=7) and Gria1−/− mice (N=7) undgo the same procedure as Experiment 1A but now they receive either vehicle or a higher dose of Eglumegad (LY354740) (30 mg/kg). Subsequently, in Experiment 1C, to investigate the potential effects of increased proactive interference, the procedure used in Experiment 1B is repeated in the same mice, using the same drug dose (30 mg/kg), but now using a modified testing protocol in which the interval between trials is reduced to 20 s.
Rats[4]
Two experiments are conducted. The first experiment compares the effects of LY354740 (10 mg/kg, i.p., neutralized to a pH ~ 7.4) or vehicle (0.9% saline neutralized to pH ~ 7.4) in rats remaining in their home cages or rats exposed to 2 h of immobilization stress in plastic cones (n=7, cage control/vehicle; n=7, cage control/LY354740; n=6, stress/vehicle; n=6, stress/Eglumegad (LY354740)). The second experiment compares two lower LY354740 doses (1 and 3 mg/kg, i.p.) or vehicle in rats exposed to a 2-h period of immobilization stress to rats treated with vehicle in their home cages (n=4 for all groups). All animals are injected with either Eglumegad (LY354740) or vehicle 15 min prior to being placed in plastic cones with the open end securely closed. All immobilized rats are placed in plexiglass chamber with animal bedding on the bottom; brought to a quiet room outside of the animal colony; and immediately placed in a plastic cone. Two hours after being placed in the plastic containers, the rats are decapitated. The brains are removed and frozen on dry ice, and stored at −80°C.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (279 KB)
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SDS (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Boerner T, et al. The group II metabotropic glutamate receptor agonist LY354740 and the D2 receptor antagonist haloperidol reduce locomotor hyperactivity but fail to rescue spatial working memory in GluA1 knockout mice. Eur J Neurosci. 2017 Apr;45(7):912- [Content Brief]
[2]. Orlando R, et al. Levels of the Rab GDP dissociation inhibitor (GDI) are altered in the prenatal restrain stress mouse model of schizophrenia and are differentially regulated by the mGlu2/3 receptor agonists, LY379268 and LY354740. Neuropharmacology. 2014 [Content Brief]
[3]. Procaccini C, et al. Reversal of novelty-induced hyperlocomotion and hippocampal c-Fos expression in GluA1 knockout male mice by the mGluR2/3 agonist LY354740. Neuroscience. 2013 Oct 10;250:189-200 [Content Brief]
[4]. Lee Y, et al. The mGlu2/3 receptor agonist LY354740 suppresses immobilization stress-induced increase in rat prefrontal cortical BDNF mRNA expression. Neurosci Lett. 2006 May 8;398(3):328-32. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 5.4002 mL | 27.0008 mL | 54.0015 mL | 135.0038 mL |
| 5 mM | 1.0800 mL | 5.4002 mL | 10.8003 mL | 27.0008 mL | |
| 10 mM | 0.5400 mL | 2.7001 mL | 5.4002 mL | 13.5004 mL | |
| 15 mM | 0.3600 mL | 1.8001 mL | 3.6001 mL | 9.0003 mL | |
| 20 mM | 0.2700 mL | 1.3500 mL | 2.7001 mL | 6.7502 mL | |
| 25 mM | 0.2160 mL | 1.0800 mL | 2.1601 mL | 5.4002 mL | |
| 30 mM | 0.1800 mL | 0.9000 mL | 1.8001 mL | 4.5001 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Eglumegad 関連分類
HY-18941 関連分類
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