NS-5806 (NS5806) is a novel and potent potassium current KV4.3 channel activator which 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 KChIP.

Physicochemical Properties

Molecular Formula	C16H8BR2F6N6O
Molecular Weight	574.07
Exact Mass	571.903
CAS #	426834-69-7
PubChem CID	11642685
Appearance	White to off-white solid powder
LogP	6.159
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	10
Rotatable Bond Count	3
Heavy Atom Count	31
Complexity	619
Defined Atom Stereocenter Count	0
InChi Key	UZWJWROOLOOCPQ-UHFFFAOYSA-N
InChi Code	InChI=1S/C16H8Br2F6N6O/c17-8-4-10(13-27-29-30-28-13)12(11(18)5-8)26-14(31)25-9-2-6(15(19,20)21)1-7(3-9)16(22,23)24/h1-5H,(H2,25,26,31)(H,27,28,29,30)
Chemical Name	1-[3,5-bis(trifluoromethyl)phenyl]-3-[2,4-dibromo-6-(2H-tetrazol-5-yl)phenyl]urea
Synonyms	NS5806 NS 5806 NS-5806
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro

In CHO-K1 cells, NS5806 (10 μM) causes a 65% increase in the concentration requirement for KV4.3/KChIP2/DPP6 peak current rising, a slowdown in the inactivation time course (τ), and an EC50 value of 25.4 μM [1]. With an IC50 of 40.7 nM and an EC50 of 1.6 nM, the canine instantaneous outward potassium current (Ito) both stimulates and inhibits rabbits [2]. Effects of NS5806 (10-100 nM) on atrial and ventricular Ito are concentration-dependent [2].

References

[1]. 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]. Differential responses of rabbit ventricular and atrial transient outward current (Ito) to the Itomodulator NS5806. Physiol Rep. 2017 Mar;5(5). pii: e13172.

Solubility Data

Solubility (In Vitro)

DMSO : ~250 mg/mL (~435.49 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.08 mg/mL (3.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.7419 mL	8.7097 mL	17.4195 mL
	5 mM	0.3484 mL	1.7419 mL	3.4839 mL
	10 mM	0.1742 mL	0.8710 mL	1.7419 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.