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NYX-2925 

Cat. No. M29106
NYX-2925  Structure
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Biological Activity

NYX-2925 is an orally active NMDAR modulator. NYX-2925 restores levels of activated Src and Src phosphorylation sites on GluN2A and GluN2B in the mPFC. NYX-2925 shows no effect on CAMKII, and any addictive or sedative/ataxic side effects. NYX-2925 can be used for research of a variety of NMDA receptor-mediated central nervous system disorders.

Chemical Information
Molecular Weight 297.35
Formula C14H23N3O4
CAS Number 2012536-16-0
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Gladys Morrison, et al. Neurobiol Pain. The NMDAR modulator NYX-2925 alleviates neuropathic pain via a Src-dependent mechanism in the mPFC

[2] M Scott Bowers, et al. J Neurochem. NYX-2925 induces metabotropic N-methyl-d-aspartate receptor (NMDAR) signaling that enhances synaptic NMDAR and α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor

[3] David R Houck, et al. Clin Transl Sci. NYX-2925, A Novel N-methyl-D-aspartate Receptor Modulator: A First-in-Human, Randomized, Double-blind Study of Safety and Pharmacokinetics in Adults

[4] Nayereh Ghoreishi-Haack, et al. J Pharmacol Exp Ther. NYX-2925 Is a Novel N-Methyl-d-Aspartate Receptor Modulator that Induces Rapid and Long-Lasting Analgesia in Rat Models of Neuropathic Pain

[5] M Amin Khan, et al. Int J Neuropsychopharmacol. NYX-2925 Is a Novel NMDA Receptor-Specific Spirocyclic-β-Lactam That Modulates Synaptic Plasticity Processes Associated with Learning and Memory

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  Catalog
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Keywords: NYX-2925  supplier, GluR, inhibitors, activators


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