2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. Eglumegad

Eglumegad  (Synonyms: LY354740; Eglumetad)

Cat. No.: HY-18941 Purity: 99.88%
COA Handling Instructions

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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.

For research use only. We do not sell to patients.

Eglumegad Chemical Structure

Eglumegad Chemical Structure

CAS No. : 176199-48-7

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in Water
ready for reconstitution
 USD 165 In-stock
Solution
10 mM * 1 mL in Water USD 165 In-stock
Solid
5 mg USD 150 In-stock
10 mg USD 250 In-stock
25 mg USD 500 In-stock
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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Eglumegad:

Eglumegad Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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.

IC50 & Target[1]

mGluR2R

5 nM (IC50)

mGluR3R

24 nM (IC50)

In Vitro

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.

Eglumegad Related Antibodies
In Vivo

Eglumegad (LY354740) (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 concentration of 30 mg/kg. Eglumegad (LY354740) (15 or 30 mg/kg, i.p.) reduces spontaneous locomotor activity in wild-type and Gria1 / mice[1]. Eglumegad (LY354740) (15 mg/kg, i.p.) dreases novelty-induced hyperlocomotion in naive GluA1-KO and pre-handled GluA1-KO males, but not in females. Eglumegad (LY354740) (15 mg/kg, i.p.) significantly reduces the increased c-Fos expression of GluA1-KO males to the level of WT males, but not in of females[3]. Eglumegad (LY354740) (10 mg/kg, i.p.) attenuates the immobilization stress-induced increase in BDNF mRNA expression in the rat mPFC[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

185.18

Formula

C8H11NO4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC([C@]1([C@]2([H])[C@@H](C(O)=O)[C@]2([H])CC1)N)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (179.99 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 6.33 mg/mL (34.18 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.4002 mL 27.0008 mL 54.0015 mL
5 mM 1.0800 mL 5.4002 mL 10.8003 mL
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (13.50 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.

  • Protocol 1

    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

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.88%

COA (247 KB) HNMR (448 KB) RP-HPLC (237 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[1][4]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

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 / DMSO 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
DMSO 40 mM 0.1350 mL 0.6750 mL 1.3500 mL 3.3751 mL
50 mM 0.1080 mL 0.5400 mL 1.0800 mL 2.7001 mL
60 mM 0.0900 mL 0.4500 mL 0.9000 mL 2.2501 mL
80 mM 0.0675 mL 0.3375 mL 0.6750 mL 1.6875 mL
100 mM 0.0540 mL 0.2700 mL 0.5400 mL 1.3500 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.

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Eglumegad Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Eglumegad176199-48-7LY354740 EglumetadLY 354740LY-354740mGluRMetabotropic glutamate receptorsInhibitorinhibitorinhibit

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