NS5806 (10 µM) induces a 65% increase of KV4.3/KChIP2/DPP6 peak current amplitudes concentration-dependently and the time course of inactivation (τ) is slowed with an EC50 value of 25.4 µM in CHO-K1 cells[1]. NS5806 activates canine transient outward potassium current (Ito) with an IC50 of 40.7 nM and an EC50 of 1.6 nM for inhibition and stimulation on rabbit, respectively[2]. NS5806 (10-100 nM) has concentration-dependent effects on ventricular and atrial Ito[2].
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Lundby A, et al. Effect of the I(to) activator NS5806 on cloned KV4 channels depends on the accessory protein KChIP2. Br J Pharmacol. 2010 Aug;160(8):2028-44. doi: 10.1111/j.1476-5381.2010.00859.x.
[2]. Cheng H, et al. Differential responses of rabbit ventricular and atrial transient outward current (Ito) to the Itomodulator NS5806. Physiol Rep. 2017 Mar;5(5). pii: e13172.
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