[CAS NO. 191471-52-0] LY379268

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PRODUCTS SPECIFICATIONS [191471-52-0]

Catalog

HY-103558

Brand

MCE

CAS

191471-52-0

DESCRIPTION [191471-52-0]

Overview

MDL	-
Molecular Weight	187.15
Molecular Formula	C7H9NO5
SMILES	O=C([C@]1(N)CO[C@@]2([H])[C@H](C(O)=O)[C@@]12[H])O

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

Summary

LY379268 is a potent, selective and brain-penetrant mGlu2/3R agonist with EC ₅₀ 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

hmGluR2

2.69 nM (EC ₅₀ )

hmGluR3

4.48 nM (EC ₅₀ )

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.

Appearance

Solid

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)

H ₂ O : 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
10 mM	0.5343 mL	2.6717 mL	5.3433 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: PBS

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

* All of the co-solvents are available by MCE.

References

Synonyms

2-Oxabicyclo[3.1.0]hexane-4,6-dicarboxylic acid, 4-amino-, (1R,4R,5S,6R)-

2-Oxabicyclo[3.1.0]hexane-4,6-dicarboxylic acid, 4-amino-, [1R-(1α,4β,5α,6α)]-

(1R,4R,5S,6R)-4-Amino-2-oxabicyclo[3.1.0]hexane-4,6-dicarboxylic acid

LY 379268