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NS 5806

Cat. No. M7052
NS 5806 Structure
Size Price Availability Quantity
5mg USD 150  USD150 In stock
10mg USD 240  USD240 In stock
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Quality Control & Documentation
Biological Activity

NS 5806 is a 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.

Chemical Information
Molecular Weight 574.07
Formula C16H8Br2F6N6O
CAS Number 426834-69-7
Solubility (25°C) DMSO 57.41 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Smith, et al. ACS Chem Neurosci. Recent advances in the design, synthesis, and biological evaluation of selective DYRK1A inhibitors: a new avenue for a disease modifying treatment of Alzheimer's?.

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Keywords: NS 5806 supplier, Potassium Channel, inhibitors, activators


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