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GIRK1/4 inhibitor 14b

Chemical Structure : GIRK1/4 inhibitor 14b

CAS No.: 2222665-46-3

GIRK1/4 inhibitor 14b

Catalog No.: PC-20299Not For Human Use, Lab Use Only.

GIRK1/4 inhibitor 14b is a potent, brain-sparing GIRK1/4 inhibitor with IC50 of 0.1 uM, exhibits excellent selectivity over GIRK1/2 channel.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

GIRK1/4 inhibitor 14b is a potent, brain-sparing GIRK1/4 inhibitor with IC50 of 0.1 uM, exhibits excellent selectivity over GIRK1/2 channel.
GIRK1/4 inhibitor 14b demonstrated targeted clinical exposure of 1.2 μM on AERP in an anesthetized guinea pig model.
GIRK1/4 inhibitor 14b treatment resulted in prolongation of the shortened AERP over a 20 to 30 min time period until steady-state was achieved.

Physicochemical Properties

M.Wt 445.68
Formula C18H15Cl3N2O5
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

(S)-8-chloro-1-(2,6-dichlorophenyl)-5-(2,3-dihydroxypropoxy)-2-(hydroxymethyl)-1,6-naphthyridin-4(1H)-one

References

1. Stefan Peukert, et al. Bioorg Med Chem Lett. 2023 Apr 1;85:129237.

2. Patent WO2022074567 A1.

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