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LY 2812223

Chemical Structure : LY 2812223

CAS No.: 1311385-20-2

LY 2812223 (LY2812223;LY-2812223)

Catalog No.: PC-60818Not For Human Use, Lab Use Only.

A highly potent, functionally selective mGlu2 receptor agonist with EC50 of 13.6 nM in GTPγS functional binding assay.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A highly potent, functionally selective mGlu2 receptor agonist with EC50 of 13.6 nM in GTPγS functional binding assay; displays little to no affinity for mGlu1, mGlu4, mGlu5 or mGlu7 receptors; fully displaces the mGlu2/3 agonist radioligand [3H]LY459477 with Ki of 118 nM, inhibits forskolin-stimulated cAMP with EC50 of 16.1 nM; displays near maximal agonist responses at the mGlu2 receptor across all assay formats, while shows no functional agonist activity at the mGlu3 receptor except in the cAMP assay.

Alzheimer Disease

Phase 2 Clinical

Physicochemical Properties

M.Wt
Formula
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(1R,2S,4R,5R,6R)-2-amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic acid

References

1. Monn JA, et al. J Med Chem. 2015 Sep 24;58(18):7526-48.

2. Felder CC, et al. J Pharmacol Exp Ther. 2017 Apr;361(1):190-197.

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