| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
NS-5806 targets the Kv4 family of voltage-gated potassium channels, specifically Kv4.3 and Kv4.2. It increases IKv4.3 peak current amplitude in CHO-K1 cells expressing KV4.3 and KChIP2 with an EC₅₀ of 5.3 μM. NS-5806 slows KV4.3 and KV4.2 current decay in channel complexes containing KChIP2. It also decays Kv4.1 independent of KChIP2 and strongly inhibits Kv1.4 at 10 μM, but has no effect on Kv7.1, Kv11.1 and K(ii)2 currents.
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| 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].
In vitro, NS-5806 increases ventricular Ito with a leftward shift in Ito activation and accelerated restitution at 10 μM. It has concentration-dependent effects on ventricular and atrial Ito at 10-100 nM. The compound directly increases the current amplitude and alters the voltage dependence of KV4.3 channels, enhancing their activation at more negative potentials. NS-5806 is used in electrophysiology studies to investigate potassium channel function. |
| ln Vivo |
In vivo, NS-5806 has been studied in animal models for its potential therapeutic applications in pain and neurological disorders. As a Kv4.3 channel activator, it modulates the transient outward potassium current (Ito) in excitable tissues. The compound's effects on neuronal excitability make it a valuable tool for studying neurological disease mechanisms. Detailed results are available in specialized pharmacological literature.
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| Enzyme Assay |
Electrophysiological patch-clamp recordings: CHO-K1 cells expressing KV4.3 and KChIP2 are cultured and subjected to whole-cell patch-clamp. NS-5806 is applied at various concentrations (typically 0.1-100 μM) in extracellular solution. Inward potassium currents are recorded and EC₅₀ values are calculated from dose-response curves. For selectivity studies, currents are recorded from cells expressing various potassium channel subtypes.
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| Cell Assay |
CHO-K1 cells stably or transiently expressing KV4.3 and KChIP2 are cultured in F-12 medium with 10% FBS at 37°C with 5% CO₂. For electrophysiology, cells are plated on coverslips and whole-cell patch-clamp recordings are performed. Cells are treated with NS-5806 at various concentrations and potassium currents are recorded. IC₅₀ and EC₅₀ values are calculated from dose-response curves.
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| Animal Protocol |
In vivo studies are conducted in rodent models of pain and neurological disorders. NS-5806 is formulated in suitable vehicles (e.g., saline, DMSO/PEG mixtures) and administered via intraperitoneal, intravenous, or other routes at specified doses. Behavioral tests are performed to assess pain responses and neurological function. Electrophysiological recordings from excitable tissues are conducted to confirm target engagement.
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| ADME/Pharmacokinetics |
NS-5806 has molecular formula C₁₆H₈Br₂F₆N₆O and molecular weight 574.07. It is soluble in DMSO (10 mM). The compound has InChI Key UZWJWROOLOOCPQ-UHFFFAOYSA-N. It is typically stored as a powder at -20°C and protected from light and moisture. Purity is ≥98%.
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| References |
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| Additional Infomation |
NS-5806 is a diaryl-urea small molecule developed as a potent activator of Kv4.3 potassium channels for the treatment of pain and neurological disorders. It is widely used to study Kv4 channel physiology in excitable cells, including trigeminal neurons. The compound's effects are critically dictated by the Kv4 family of voltage-gated potassium channels. It is intended for research purposes only and is not approved for human use.
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| Molecular Formula |
C16H8BR2F6N6O
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|---|---|
| Molecular Weight |
574.07
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| Exact Mass |
571.903
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| CAS # |
426834-69-7
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| PubChem CID |
11642685
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| Appearance |
White to off-white solid powder
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| LogP |
6.159
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
31
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| Complexity |
619
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
UZWJWROOLOOCPQ-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
1-[3,5-bis(trifluoromethyl)phenyl]-3-[2,4-dibromo-6-(2H-tetrazol-5-yl)phenyl]urea
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| Synonyms |
NS5806 NS 5806 NS-5806
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~435.49 mM)
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| 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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