LY 2812223( LY2812223 | LY-2812223 )

Catalog No. M11252 CAS No. 1311385-20-2

COA

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HNMR

HPLC

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Product Name

LY 2812223
Note

Research use only, not for human use.
Brief Description

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

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.
In Vitro

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In Vivo

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Synonyms

LY2812223 | LY-2812223
Pathway

GPCR/G Protein
Target

mGluR
Recptor

mGluR
Research Area

Neurological Disease
Indication

Alzheimer Disease

CAS Number

1311385-20-2
Formula Weight

835.828
Molecular Formula

——
Purity

>98% (HPLC)
Solubility

In Vitro:?H2O : 50 mg/mL (175.88 mM)
SMILES

[H][C@]12[C@]([C@H]2C(O)=O)([H])[C@@](C(O)=O)(N)C[C@H]1SC3=NNC=N3
Chemical Name

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

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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