NS8593 hydrochloride

Research use only, not for human use.

NS8593 hydrochloride is a potent and selective inhibitor of small conductance Ca2+-activated K+ channels (SK channels) .

NS8593 hydrochloride is a potent and selective inhibitor of small conductance Ca2+-activated K+ channels (SK channels) .

When tested in excised patches, it is found that the inhibition by NS8593 (compound 14) decreased as the intracellular [Ca2+] is increased and that NS8593 is equipotent when applied from either the intracellular or the extracellular side of the cell membrane. A HEK293 cell transiently transfected with hSK3 channels is inhibited by 80% upon application of 100 nM apamin and by 75% after application of 300 nM NS8593. In contrast, NS8593 inhibits the mutated channel by 45% at 300 nM. NS8593 thus remains active on the apamin-insensitive SK3 channel, although the Kd value of 0.43 μM is 4-fold higher than found for a wild-type hSK3 channel (Kd of 0.10 μM). As the potency of NS8593 is dependent on the degree of SK3 channel activation, the decreased potency could thus reflect an increased apparent Ca2+-sensitivity of the mutated channels. Similar to the whole-cell experiments, the potency of NS8593 is reduced 3-fold from 0.67 μM to 2.2 μM when tested at a Ca2+ concentration of 500 nM.

NS8593 (compound 14) (3 and 10 mg/kg intravenously) is able to affect firing rate and firing pattern of dopaminergic neurons in vivo in C57Bl/6 mice.

NS8593 HCl

Cell Cycle/DNA Damage

Potassium Channel

SK channel

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875755-24-1

299.8

C17H18ClN3

>98% (HPLC)

DMSO:80 mg/mL?(266.84 mM;?Need ultrasonic)

[H]Cl.C1(N[C@@H]2CCCC3=C2C=CC=C3)=NC4=CC=CC=C4N1

——

(-20℃)

With Ice Pack

≥ 2 years