2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. LY379268

LY379268 is a potent, selective and brain-penetrant mGlu2/3R agonist with EC50 values of 2.69 nM (mGlu2) and 4.48 nM (mGlu3). LY379268 has no activity on human mGlu 1a, 4a, 5a or 7a receptors. LY379268 has antioxidant and neuroprotective effects.

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LY379268 Chemical Structure

LY379268 Chemical Structure

CAS No. : 191471-52-0

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Based on 1 publication(s) in Google Scholar

LY379268 Related Antibodies

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Description

LY379268 is a potent, selective and brain-penetrant mGlu2/3R agonist with EC50 values of 2.69 nM (mGlu2) and 4.48 nM (mGlu3). LY379268 has no activity on human mGlu 1a, 4a, 5a or 7a receptors. LY379268 has antioxidant and neuroprotective effects[1][2].

IC50 & Target[1]

hmGluR2

2.69 nM (EC50)

hmGluR3

4.48 nM (EC50)

hmGluR2

14.1 nM (Ki)

hmGluR3

5.8 nM (Ki)

In Vitro

Treatment of 9-weeks (9w) astrocytes with LY379268 (0.1 μM; 24-48 hours) results in an increase in mGlu3R and Nrf2 protein levels and SOD activity, and decreases mitochondrial ROS levels and apoptosis. mGlu3R activation in aged astrocytes also preventS hippocampal neuronal death induced by Aβ1-42 in co-culture assays. Activation of mGlu3R in aged astrocytes haS an anti-oxidant effect and protected hippocampal neurons against Aβ-induced neurotoxicity[3].

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

LY379268 Related Antibodies
In Vivo

For LY379268, when a 3 mg/kg dose is given prior to an intraplantar injection of carrageenan, the inflammatory hyperalgesia that developed is significantly delayed, without affecting the inflammation of the paw[2].
In a model of mouse tail withdrawal to warm water, LY379268 (12 mg/kg; i.p.), given before a subcutaneous tail injection of capsaicin, reduces the subsequent neurogenic hyperalgesia[2].

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

187.15

Formula

C7H9NO5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@]1(N)CO[C@@]2([H])[C@H](C(O)=O)[C@@]12[H])O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

0.1 M NaOH : 200 mg/mL (1068.66 mM; ultrasonic and adjust pH to 8 with NaOH)

H2O : 2 mg/mL (10.69 mM; ultrasonic and adjust pH to 10 with NaOH)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.3433 mL 26.7165 mL 53.4331 mL
5 mM 1.0687 mL 5.3433 mL 10.6866 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* 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:

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: 25 mg/mL (133.58 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working 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).
Purity & Documentation

Purity: 99.84% ee.: 99.32%

COA (253 KB) HNMR (208 KB) RP-HPLC (254 KB) NP-HPLC (611 KB)

Handling Instructions (2659 KB)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / 0.1 M NaOH 1 mM 5.3433 mL 26.7165 mL 53.4331 mL 133.5827 mL
5 mM 1.0687 mL 5.3433 mL 10.6866 mL 26.7165 mL
10 mM 0.5343 mL 2.6717 mL 5.3433 mL 13.3583 mL
0.1 M NaOH 15 mM 0.3562 mL 1.7811 mL 3.5622 mL 8.9055 mL
20 mM 0.2672 mL 1.3358 mL 2.6717 mL 6.6791 mL
25 mM 0.2137 mL 1.0687 mL 2.1373 mL 5.3433 mL
30 mM 0.1781 mL 0.8906 mL 1.7811 mL 4.4528 mL
40 mM 0.1336 mL 0.6679 mL 1.3358 mL 3.3396 mL
50 mM 0.1069 mL 0.5343 mL 1.0687 mL 2.6717 mL
60 mM 0.0891 mL 0.4453 mL 0.8906 mL 2.2264 mL
80 mM 0.0668 mL 0.3340 mL 0.6679 mL 1.6698 mL
100 mM 0.0534 mL 0.2672 mL 0.5343 mL 1.3358 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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LY379268 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:

LY379268191471-52-0LY 379268LY-379268mGluRMetabotropic glutamate receptorsmGlu3RmGlu2RNrf2ROSSODantioxidantneuroprotectiveInhibitorinhibitorinhibit

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