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Eglumegad

Catalog No. T15817 CAS 176199-48-7

Synonyms: 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, CAS 176199-48-7

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	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).
Targets&IC50	mGluR2R:5 nM (IC50), mGluR3R:24 nM (IC50)
In vitro	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].
In vivo	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].

Synonyms	Eglumetad, LY354740
Molecular Weight	185.18
Formula	C8H11NO4
CAS No.	176199-48-7

Storage

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

Solubility Information

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

References and Literature

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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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

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

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