NS 1643An antiarrhythmic activator of hERG K+ channels

NS 1643 (CAS 448895-37-2)

NS 1643 | CAS 448895-37-2 is rated 5.0 out of 5 by 1.
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Synonym: N,N'-Bis[2-hydroxy-5-(trifluoromethyl)phenyl] urea
Application: An antiarrhythmic activator of hERG K+ channels
CAS Number: 448895-37-2
Molecular Weight: 380.25
Molecular Formula: C15H10F6N2O3
Supplemental Information: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
* Refer to Certificate of Analysis for lot specific data (including water content).
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NS 1643 is a HERG(hERG K+ channel) activator, such as KCNH6. Displays different molecular mechanisms of action at hERG1 and hERG2 channels. Exhibits antiarrhythmic activity in vitro.


References

Hansen et al (2006) Activation of human ether-a-go-go related gene potassium channels by the diphenylurea 1,3-bis-(2-hydroxy-5-trifluoromethyl-phenyl)-urea (NS1643). Mol.Pharmacol. 69 266. Casis et al (2006) Mechanism of action of a novel human ether-a-go-ao related gene channel activator. Mol.Pharmacol. 69 658. Elmedyb et al (2007) Activation of ERG2 potassium channel by the diphenylurea NS1643. Neuropharmacology 53 283.

Physical State :
Solid
Solubility :
Soluble in ethanol (100 mM), and DMSO (≥20 mg/ml).
Storage :
Store at -20° C
Melting Point :
191.57° C (Predicted)
Boiling Point :
~342.31° C at 760 mmHg (Predicted)
Density :
~1.6 g/cm3 (Predicted)
Refractive Index :
n20D 1.59 (Predicted)
IC50 :
Activated HERG KV11.1 channel : EC5050 = 10.5 µM (human)
pK Values :
pKa: 6.84 (Predicted), pKb: 1.14 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
10177784
MDL Number :
MFCD08705418
SMILES :
C1=CC(=C(C=C1C(F)(F)F)NC(=O)NC2=C(C=CC(=C2)C(F)(F)F)O)O

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NS 1643  Product Citations

See how others have used NS 1643. Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 27470144  Sala, L. et al. 2016. EMBO Mol Med. 8: 1065-81.

PMID: # 28163191  Kitaguchi, T. et al. J Pharmacol Toxicol Methods. 85: 73-81.

Citations 1 to 2 of 2 total
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Rated 5 out of 5 by from Lansu et al Lansu et al. (PubMed ID 23744352) found that the hERG1 channel activator, NS1643, inhibited breast cancer cell proliferation irreversibly by inducing cell cycle arrest in G0/G1 phase. -SCBT Publication Review
Date published: 2015-06-16
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