| Bioactivity | NS5806, a potent potassium current activator, increases KV4.3/KChIP2 peak current amplitudes with an EC50 of 5.3 μM. NS5806 slows KV4.3 and KV4.2 current dacay in channel complexes containing KChIP2[1]. | |||||||||
| Target | IC50: 5.3 nM (KV4.3) | |||||||||
| Invitro | 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]. | |||||||||
| Name | NS5806 | |||||||||
| CAS | 426834-69-7 | |||||||||
| Formula | C16H8Br2F6N6O | |||||||||
| Molar Mass | 574.07 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [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. |