Biological Activity
KV4.3 channel activator; mediates the transient outward K+ current (Ito). Increases IKv4.3 peak current amplitude in CHO-K1 cells expressing KV4.3 and KChIP2 (EC50 = 5.3 μM). Inhibits KV1.4-mediated currents independently of KChIP2. Also slows the decay of KV4.2 and KV4.3 currents in the presence of KChIP2.
Compound Libraries
NS 5806 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
M. Wt | 574.07 |
Formula | C16H8Br2F6N6O |
Storage | Store at +4°C |
Purity | ≥99% (HPLC) |
CAS Number | 426834-69-7 |
PubChem ID | 11642685 |
InChI Key | UZWJWROOLOOCPQ-UHFFFAOYSA-N |
Smiles | BrC1=CC(Br)=CC(C2=NN=NN2)=C1NC(NC3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 57.41 | 100 | |
ethanol | 28.7 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 574.07. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.74 mL | 8.71 mL | 17.42 mL |
5 mM | 0.35 mL | 1.74 mL | 3.48 mL |
10 mM | 0.17 mL | 0.87 mL | 1.74 mL |
50 mM | 0.03 mL | 0.17 mL | 0.35 mL |
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References
References are publications that support the products' biological activity.
Calloe et al (2009) A transient outward potassium current activator recapitulates the electrocardiographic manifestations of Brugada syndrome. Cardiovasc.Res. 81 686 PMID: 19073629
Calloe et al (2010) Differential effects of the transient outward K+ current activator NS5806 in the canine left ventricle. J.Mol.Cell.Cardiol. 48 191 PMID: 19632239
Lundby et al (2010) Effect of the Ito activator NS5806 on cloned Kv4 channels depends on the accessory protein KChIP2. Br.J.Pharmacol. 160 2028 PMID: 20649599
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