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Eglumegad

Eglumegad

产品编号 T15817   CAS 176199-48-7
别名: Eglumetad, LY354740

Eglumegad is a highly effective and selective agonist of group II (mGlu2/3) receptor (IC50s: 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively).

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Eglumegad Chemical Structure
Eglumegad, CAS 176199-48-7
规格 价格/CNY 货期 数量
2 mg ¥ 888 5日内发货
5 mg ¥ 824 5日内发货
药物设计专题培训
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
产品目录号及名称: Eglumegad (T15817)
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参考文献
产品描述 Eglumegad is a highly effective and selective agonist of group II (mGlu2/3) receptor (IC50s: 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively).
靶点活性 mGluR2R:5 nM (IC50), mGluR3R:24 nM (IC50)
体外活性 In mouse cortical neurons, Eglumegad 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). It also up-regulates spot 6507 (collapsin response mediator protein 1)[2].
体内活性 Eglumegad (15 or 30 mg/kg, i.p.) has no effect on spatial working memory performance in Gria1?/? or WT mice, and it has no effect on rewarded alternation testing with a short inter-trial interval in Gria1?/? and WT mice at a concentration of 30 mg/kg and it decreases spontaneous locomotor activity in wild-type and Gria1?/? mice[1]. Eglumegad (15 mg/kg, i.p.) reduces novelty-induced hyperlocomotion in naive GluA1-KO and pre-handled GluA1-KO males, but not in females and it also significantly reduces the increased c-Fos expression of GluA1-KO males to the level of WT males, but not in females[3]. Eglumegad (10 mg/kg, i.p.) attenuates the immobilization stress-induced increase in BDNF mRNA expression in the rat mPFC[4].
别名 Eglumetad, LY354740
分子量 185.18
分子式 C8H11NO4
CAS No. 176199-48-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: 6.33 mg/mL (34.18 mM), Sonication and heating are recommended.

溶液配制表

可选溶剂 浓度 体积 质量 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 1.08 mL 5.4002 mL 10.8003 mL 27.0008 mL
10 mM 0.54 mL 2.7001 mL 5.4002 mL 13.5004 mL
20 mM 0.27 mL 1.35 mL 2.7001 mL 6.7502 mL

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TargetMol Library Books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- 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 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 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.

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

Eglumegad 176199-48-7 Others Eglumetad LY-354740 LY354740 LY 354740 Inhibitor inhibitor inhibit

 

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