Cas No.: | 426834-69-7 |
Chemical Name: | N-[3,5-Bis(trifluoromethyl)phenyl]-N'-[2,4-dibromo-6-(2H-tetrazol-5-yl)phenyl]urea |
Synonyms: | NS5806;NS-5806;NS 5806 |
SMILES: | BrC1=CC(Br)=C(NC(NC2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2)=O)C(C2N=NNN=2)=C1 |
Formula: | C16H8Br2F6N6O |
M.Wt: | 574.07 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Publication: | [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. |
Description: | 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)[1] |
In Vitro: | 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]. |
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. |