NS-5806
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MedKoo CAT#: 563519

CAS#: 426834-69-7

Description: NS-5806 is a KV4.3 channel activator. It acts by mediating the transient outward K+ current (Ito) and increasing IKv4.3 peak current amplitude in CHO-K1 cells expressing KV4.3 and KChIP2.


Price and Availability

Size Price Shipping out time Quantity
5mg USD 290 2 Weeks
25mg USD 720 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-08-03. Prices are subject to change without notice.

NS-5806, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 563519
Name: NS-5806
CAS#: 426834-69-7
Chemical Formula: C16H8Br2F6N6O
Exact Mass: 571.9031
Molecular Weight: 574.07
Elemental Analysis: C, 33.48; H, 1.40; Br, 27.84; F, 19.86; N, 14.64; O, 2.79


Synonym: NS-5806; NS 5806; NS5806;

IUPAC/Chemical Name: 1-[3,5-Bis(trifluoromethyl)phenyl]-3-[2,4-dibromo-6-(2H-tetrazol-5-yl)phenyl]urea

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)

SMILES Code: O=C(NC1=C(C2=NNN=N2)C=C(Br)C=C1Br)NC3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>3 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.03.00


References

1: Patocskai B, Yoon N, Antzelevitch C. Mechanisms Underlying Epicardial Radiofrequency Ablation to Suppress Arrhythmogenesis in Experimental Models of Brugada Syndrome. JACC Clin Electrophysiol. 2017 Apr;3(4):353-363. doi: 10.1016/j.jacep.2016.10.011. Epub 2016 Dec 21. PubMed PMID: 28948234; PubMed Central PMCID: PMC5609479.

2: Cheng H, Cannell MB, Hancox JC. Differential responses of rabbit ventricular and atrial transient outward current (I(to)) to the I(to) modulator NS5806. Physiol Rep. 2017 Mar;5(5). pii: e13172. doi: 10.14814/phy2.13172. PubMed PMID: 28270595; PubMed Central PMCID: PMC5350179.

3: Wu KW, Kou ZW, Mo JL, Deng XX, Sun FY. Neurovascular coupling protects neurons against hypoxic injury via inhibition of potassium currents by generation of nitric oxide in direct neuron and endothelium cocultures. Neuroscience. 2016 Oct 15;334:275-282. doi: 10.1016/j.neuroscience.2016.08.012. Epub 2016 Aug 12. PubMed PMID: 27531855.

4: Gonzalez WG, Ramos V, Diaz M, Garabedian A, Molano-Arevalo JC, Fernandez-Lima F, Miksovska J. Characterization of the Photophysical, Thermodynamic, and Structural Properties of the Terbium(III)-DREAM Complex. Biochemistry. 2016 Mar 29;55(12):1873-86. doi: 10.1021/acs.biochem.6b00067. Epub 2016 Mar 7. PubMed PMID: 26901070; PubMed Central PMCID: PMC4867112.

5: Patocskai B, Barajas-Martinez H, Hu D, Gurabi Z, Koncz I, Antzelevitch C. Cellular and ionic mechanisms underlying the effects of cilostazol, milrinone, and isoproterenol to suppress arrhythmogenesis in an experimental model of early repolarization syndrome. Heart Rhythm. 2016 Jun;13(6):1326-34. doi: 10.1016/j.hrthm.2016.01.024. Epub 2016 Jan 25. PubMed PMID: 26820510; PubMed Central PMCID: PMC4879023.

6: Maleckar MM, Lines GT, Koivumäki JT, Cordeiro JM, Calloe K. NS5806 partially restores action potential duration but fails to ameliorate calcium transient dysfunction in a computational model of canine heart failure. Europace. 2014 Nov;16 Suppl 4:iv46-iv55. doi: 10.1093/europace/euu252. PubMed PMID: 25362170.

7: Gonzalez WG, Pham K, Miksovska J. Modulation of the voltage-gated potassium channel (Kv4.3) and the auxiliary protein (KChIP3) interactions by the current activator NS5806. J Biol Chem. 2014 Nov 14;289(46):32201-13. doi: 10.1074/jbc.M114.577528. Epub 2014 Sep 16. PubMed PMID: 25228688; PubMed Central PMCID: PMC4231695.

8: Szél T, Antzelevitch C. Abnormal repolarization as the basis for late potentials and fractionated electrograms recorded from epicardium in experimental models of Brugada syndrome. J Am Coll Cardiol. 2014 May 20;63(19):2037-45. doi: 10.1016/j.jacc.2014.01.067. Epub 2014 Mar 19. PubMed PMID: 24657694; PubMed Central PMCID: PMC4024366.

9: Gurabi Z, Koncz I, Patocskai B, Nesterenko VV, Antzelevitch C. Cellular mechanism underlying hypothermia-induced ventricular tachycardia/ventricular fibrillation in the setting of early repolarization and the protective effect of quinidine, cilostazol, and milrinone. Circ Arrhythm Electrophysiol. 2014 Feb;7(1):134-42. doi: 10.1161/CIRCEP.113.000919. Epub 2014 Jan 15. PubMed PMID: 24429494; PubMed Central PMCID: PMC3951442.

10: Koncz I, Gurabi Z, Patocskai B, Panama BK, Szél T, Hu D, Barajas-Martínez H, Antzelevitch C. Mechanisms underlying the development of the electrocardiographic and arrhythmic manifestations of early repolarization syndrome. J Mol Cell Cardiol. 2014 Mar;68:20-8. doi: 10.1016/j.yjmcc.2013.12.012. Epub 2013 Dec 28. PubMed PMID: 24378566; PubMed Central PMCID: PMC3943882.

11: Szél T, Koncz I, Antzelevitch C. Cellular mechanisms underlying the effects of milrinone and cilostazol to suppress arrhythmogenesis associated with Brugada syndrome. Heart Rhythm. 2013 Nov;10(11):1720-7. doi: 10.1016/j.hrthm.2013.07.047. Epub 2013 Aug 1. PubMed PMID: 23911896; PubMed Central PMCID: PMC3825770.

12: Minoura Y, Panama BK, Nesterenko VV, Betzenhauser M, Barajas-Martínez H, Hu D, Di Diego JM, Antzelevitch C. Effect of Wenxin Keli and quinidine to suppress arrhythmogenesis in an experimental model of Brugada syndrome. Heart Rhythm. 2013 Jul;10(7):1054-62. doi: 10.1016/j.hrthm.2013.03.011. Epub 2013 Mar 14. PubMed PMID: 23499631; PubMed Central PMCID: PMC3702731.

13: Witzel K, Fischer P, Bähring R. Hippocampal A-type current and Kv4.2 channel modulation by the sulfonylurea compound NS5806. Neuropharmacology. 2012 Dec;63(8):1389-403. doi: 10.1016/j.neuropharm.2012.08.017. Epub 2012 Aug 30. PubMed PMID: 22964468.

14: Cordeiro JM, Calloe K, Moise NS, Kornreich B, Giannandrea D, Di Diego JM, Olesen SP, Antzelevitch C. Physiological consequences of transient outward K+ current activation during heart failure in the canine left ventricle. J Mol Cell Cardiol. 2012 Jun;52(6):1291-8. doi: 10.1016/j.yjmcc.2012.03.001. Epub 2012 Mar 11. PubMed PMID: 22434032; PubMed Central PMCID: PMC3401930.

15: Minge D, Bähring R. Acute alterations of somatodendritic action potential dynamics in hippocampal CA1 pyramidal cells after kainate-induced status epilepticus in mice. PLoS One. 2011;6(10):e26664. doi: 10.1371/journal.pone.0026664. Epub 2011 Oct 24. PubMed PMID: 22039527; PubMed Central PMCID: PMC3200351.

16: Minoura Y, Di Diego JM, Barajas-Martínez H, Zygmunt AC, Hu D, Sicouri S, Antzelevitch C. Ionic and cellular mechanisms underlying the development of acquired Brugada syndrome in patients treated with antidepressants. J Cardiovasc Electrophysiol. 2012 Apr;23(4):423-32. doi: 10.1111/j.1540-8167.2011.02196.x. Epub 2011 Oct 28. PubMed PMID: 22034916; PubMed Central PMCID: PMC3468832.

17: Calloe K, Nof E, Jespersen T, Di Diego JM, Chlus N, Olesen SP, Antzelevitch C, Cordeiro JM. Comparison of the effects of a transient outward potassium channel activator on currents recorded from atrial and ventricular cardiomyocytes. J Cardiovasc Electrophysiol. 2011 Sep;22(9):1057-66. doi: 10.1111/j.1540-8167.2011.02053.x. Epub 2011 Apr 1. PubMed PMID: 21457383; PubMed Central PMCID: PMC3136585.

18: Lundby A, Jespersen T, Schmitt N, Grunnet M, Olesen SP, Cordeiro JM, Calloe K. Effect of the I(to) activator NS5806 on cloned K(V)4 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. PubMed PMID: 20649599; PubMed Central PMCID: PMC2958647.

19: Calloe K, Soltysinska E, Jespersen T, Lundby A, Antzelevitch C, Olesen SP, Cordeiro JM. Differential effects of the transient outward K(+) current activator NS5806 in the canine left ventricle. J Mol Cell Cardiol. 2010 Jan;48(1):191-200. doi: 10.1016/j.yjmcc.2009.07.017. Epub 2009 Jul 24. PubMed PMID: 19632239; PubMed Central PMCID: PMC2813348.

20: Calloe K, Cordeiro JM, Di Diego JM, Hansen RS, Grunnet M, Olesen SP, Antzelevitch C. A transient outward potassium current activator recapitulates the electrocardiographic manifestations of Brugada syndrome. Cardiovasc Res. 2009 Mar 1;81(4):686-94. doi: 10.1093/cvr/cvn339. Epub 2008 Dec 10. PubMed PMID: 19073629; PubMed Central PMCID: PMC2642600.