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LBG20304

Chemical Structure : LBG20304

CAS No.:

LBG20304 (LBG 20304)

Catalog No.: PC-22950Not For Human Use, Lab Use Only.

LBG20304 is a potent, selective ligand for homomeric GluK5 receptor with IC50 of 432 nM, >40-fold selective over GluK1-3 and >100-fold selectivity over native AMPA and NMDA receptors.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

LBG20304 is a potent, selective ligand for homomeric GluK5 receptor with IC50 of 432 nM, >40-fold selective over GluK1-3 and >100-fold selectivity over native AMPA and NMDA receptors.
LBG20304 interacts with the GluK5 orthosteric binding pocket.
LBG20304 (10 uM) does not activate the GluK2/5 receptor complex, does not antagonize these receptors after activation by Glu.
LBG20304 (10 and 100 μM) is a weak agonist in native murine receptors in hippocampal neurons known to express heteromeric GluK2/5 receptors.

Physicochemical Properties

M.Wt 382.38
Formula C19H18N4O5
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
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Solubility

10 mM in DMSO

Chemical Name/SMILES

(2S,3R,4R)-3-(Carboxymethyl)-4-(5-(6-hydroxynaphthalen-2-yl)-1H-1,2,3-triazol-1-yl)pyrrolidine-2-carboxylic Acid

References

1. Buschbom-Helmke S, et al. J Med Chem. 2024 Aug 12. doi: 10.1021/acs.jmedchem.4c01311.

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