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GSK3β-Nav1.6 inhibitor 1063

Chemical Structure : GSK3β-Nav1.6 inhibitor 1063

CAS No.: 321530-08-9

GSK3β-Nav1.6 inhibitor 1063

Catalog No.: PC-25144Not For Human Use, Lab Use Only.

GSK3β-Nav1.6 inhibitor 1063 is a brain-penetrant small molecule that selectively disrupts GSK3β/Nav1.6 complex formation (IC50=26.2 uM) and inhibits Nav1.6 currents in an isoform-specific manner.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

GSK3β-Nav1.6 inhibitor 1063 is a brain-penetrant small molecule that selectively disrupts GSK3β/Nav1.6 complex formation (IC50=26.2 uM) and inhibits Nav1.6 currents in an isoform-specific manner.
Compound 1063 is functionally specific for Nav1.6 over other central nervous system (CNS) Nav isoforms.
Compound 1063 reduces hippocampal hyperexcitability through a GSK3β-dependent mechanism and dose-dependently suppresses epileptiform spikes in early-stage AD mouse models.

Physicochemical Properties

M.Wt 338.47
Formula C17H26N2O3S
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

ethyl 2-(2-(isopropylamino)acetamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxylate

References

1. Baumgartner TJ, et al. Alzheimers Dement. 2025 Jul;21(7):e70507.

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