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

LY379268 

Cat. No.: HY-103558
Handling Instructions

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.

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

LY379268 Chemical Structure

LY379268 Chemical Structure

CAS No. : 191471-52-0

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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].

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

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]. LY354740 prevents release of glutamate in the striatum in freely moving rats and to attenuate morphine withdrawal-associated activation of locus coeruleus neurones, thought to be caused by an increased release of glutamate[2].

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

Molecular Weight

187.15

Formula

C₇H₉NO₅

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Product Name:
LY379268
Cat. No.:
HY-103558
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