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Zelquistinel

Chemical Structure : Zelquistinel

CAS No.: 2151842-64-5

Zelquistinel (AGN-241751, GATE-251)

Catalog No.: PC-21853Not For Human Use, Lab Use Only.

Zelquistinel (AGN-241751) is an orally active NMDAR allosteric modulator, exhibits antidepressant-like activity via positive modulation of GluN2B containing NMDARs in mPFC excitatory neurons.

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Biological Activity

Zelquistinel (AGN-241751) is an orally active NMDAR allosteric modulator, exhibits antidepressant-like activity via positive modulation of GluN2B containing NMDARs in mPFC excitatory neurons.
Zelquistinel (AGN-241751) (3-60 nM) potentiated NMDA-induced [Ca2+]i and inhibited responses at concentrations ≥100 nM, potentiates NMDA- or glutamate-induced changes in intracellular calcium.
Zelquistinel (AGN-241751), co-applied with NMDA, increases intracellular calcium in the presence of MDL 105,519.
Zelquistinel (AGN-241751) potentiates NMDAR-mediated excitatory postsynaptic currents and facilitates long-term potentiation in mPFC.
Zelquistinel (AGN-241751) dose-dependently produces and long-lasting antidepressant-like response, restores social approach behavior in stress-susceptible mice.

Physicochemical Properties

M.Wt 327.38
Formula C15H25N3O5
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

2,5-Diazaspiro[3.4]octane-5-carboxylic acid, 2-[(1S,2R)-1-(aminocarbonyl)-2-hydroxypropyl]-1-oxo-, 1,1-dimethylethyl ester, (4S)-

References

1. Burgdorf JS, et al. Int J Neuropsychopharmacol. 2022 Dec 12;25(12):979-991.

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