NS1643

• CAT Number: I003583
• CAS Number: 448895-37-2
• Molecular Formula: C15H10F6N2O3
• Molecular Weight: 380.2
• Purity: ≥95%
• Synonyms: 1,3-bis(2-hydroxy-5-(trifluoromethyl)phenyl)urea
• Target: Potassium Channel
• Solubility: 10 mM in DMSO
• Storage: Store at +4C
• InChI: InChI=1S/C15H10F6N2O3/c16-14(17,18)7-1-3-11(24)9(5-7)22-13(26)23-10-6-8(15(19,20)21)2-4-12(10)25/h1-6,24-25H,(H2,22,23,26)
• InChIKey: NJFVQMRYJZHGME-UHFFFAOYSA-N
• SMILES: OC1=C(C=C(C=C1)C(F)(F)F)NC(NC2=CC(C(F)(F)F)=CC=C2O)=O

NS1643 (Cat.No:I003583) is a small molecule compound that acts as a potent modulator of ion channels, specifically the voltage-gated potassium channels. It has been studied for its potential in treating various neurological disorders, including epilepsy and neuropathic pain. NS1643 exhibits the ability to enhance channel activity and holds promise as a therapeutic target for neurological conditions.

Reference

1:Kinetic model for NS1643 drug activation of WT and L529I variants of Kv11.1 (hERG1) potassium channel. Perissinotti LL, Guo J, De Biase PM, Clancy CE, Duff HJ, Noskov SY.Biophys J. 2015 Mar 24;108(6):1414-24. doi: 10.1016/j.bpj.2014.12.056. PMID: 25809254 Free PMC Article2:NS1643 interacts around L529 of hERG to alter voltage sensor movement on the path to activation. Guo J, Cheng YM, Lees-Miller JP, Perissinotti LL, Claydon TW, Hull CM, Thouta S, Roach DE, Durdagi S, Noskov SY, Duff HJ.Biophys J. 2015 Mar 24;108(6):1400-13. doi: 10.1016/j.bpj.2014.12.055. PMID: 25809253 Free PMC Article3:The human ether-a-go-go-related gene activator NS1643 enhances epilepsy-associated KCNQ channels. Li P, Chen X, Zhang Q, Zheng Y, Jiang H, Yang H, Gao Z.J Pharmacol Exp Ther. 2014 Dec;351(3):596-604. doi: 10.1124/jpet.114.217703. Epub 2014 Sep 17. PMID: 25232191 Free Article4:Effects of the small molecule HERG activator NS1643 on Kv11.3 channels. Bilet A, Bauer CK.PLoS One. 2012;7(11):e50886. doi: 10.1371/journal.pone.0050886. Epub 2012 Nov 30. PMID: 23226420 Free PMC Article5:Structure-guided topographic mapping and mutagenesis to elucidate binding sites for the human ether-a-go-go-related gene 1 potassium channel (KCNH2) activator NS1643. Durdagi S, Guo J, Lees-Miller JP, Noskov SY, Duff HJ.J Pharmacol Exp Ther. 2012 Aug;342(2):441-52. doi: 10.1124/jpet.111.189159. Epub 2012 May 9. PMID: 22573844 Free Article6:Strong activation of ether-à-go-go-related gene 1 K+ channel isoforms by NS1643 in human embryonic kidney 293 and Chinese hamster ovary cells. Schuster AM, Glassmeier G, Bauer CK.Mol Pharmacol. 2011 Nov;80(5):930-42. doi: 10.1124/mol.111.071621. Epub 2011 Aug 19. PMID: 21856740 Free Article7:Molecular determinants of human ether-à-go-go-related gene 1 (hERG1) K+ channel activation by NS1643. Grunnet M, Abbruzzese J, Sachse FB, Sanguinetti MC.Mol Pharmacol. 2011 Jan;79(1):1-9. doi: 10.1124/mol.110.067728. Epub 2010 Sep 27. PMID: 20876384 Free PMC Article8:Potent activation of large-conductance Ca2+-activated K+ channels by the diphenylurea 1,3-bis-[2-hydroxy-5-(trifluoromethyl)phenyl]urea (NS1643) in pituitary tumor (GH3) cells. Wu SN, Peng H, Chen BS, Wang YJ, Wu PY, Lin MW.Mol Pharmacol. 2008 Dec;74(6):1696-704. doi: 10.1124/mol.108.049106. Epub 2008 Sep 22. PMID: 18809671 Free Article9:Computational analysis of the effects of the hERG channel opener NS1643 in a human ventricular cell model. Peitersen T, Grunnet M, Benson AP, Holden AV, Holstein-Rathlou NH, Olesen SP.Heart Rhythm. 2008 May;5(5):734-41. doi: 10.1016/j.hrthm.2008.02.026. Epub 2008 Mar 4. PMID: 18452879 10:Probing the binding sites and mechanisms of action of two human ether-a-go-go-related gene channel activators, 1,3-bis-(2-hydroxy-5-trifluoromethyl-phenyl)-urea (NS1643) and 2-[2-(3,4-dichloro-phenyl)-2,3-dihydro-1H-isoindol-5-ylamino]-nicotinic acid (PD307243). Xu X, Recanatini M, Roberti M, Tseng GN.Mol Pharmacol. 2008 Jun;73(6):1709-21. doi: 10.1124/mol.108.045591. Epub 2008 Mar 27. Erratum in: Mol Pharmacol. 2008 Jul;74(1):307. PMID: 18372399 Free PMC Article