N0663
NS1643
≥98% (HPLC), solid
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About This Item
Empirical Formula (Hill Notation):
C15H10F6N2O3
CAS Number:
Molecular Weight:
380.24
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Quality Level
assay
≥98% (HPLC)
form
solid
color
white to off-white
solubility
DMSO: ≥20 mg/mL
storage temp.
2-8°C
SMILES string
Oc1ccc(cc1NC(=O)Nc2cc(ccc2O)C(F)(F)F)C(F)(F)F
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)
InChI key
NJFVQMRYJZHGME-UHFFFAOYSA-N
Biochem/physiol Actions
NS1643 is ether-a-go-go (ERG) channel activator with EC50 = 10.5 μM in Xenopus oocytes and hERG channels expressed in HEK293 cells.
The new diphenylurea compound 1,3-bis-(2-hydroxy-5-trifluoromethyl-phenyl)-urea (NS1643) was tested in hERG channel. In Xenopus laevis oocytes, NS1643 increased both steady-state and tail current at all voltages tested. The EC50 value for hERG channel activation was 10.5 μM. The effect could be reverted by application of the specific hERG channel inhibitor 4′-[[1-[2-(6-methyl-2-pyridyl)ethyl]-4-piperidinyl]carbonyl]-methanesulfonanilide (E-4031) at 100 nM. Application of NS1643 also resulted in a prolonged postrepolarization refractory time. hERG channel activation by small molecules such as NS1643 increases the repolarization reserve and presents a new antiarrhythmic approach.
Features and Benefits
This compound is featured on the Potassium Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
signalword
Danger
hcodes
Hazard Classifications
Acute Tox. 3 Oral - Eye Irrit. 2
Storage Class
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
dust mask type N95 (US), Eyeshields, Faceshields, Gloves
Regulatory Information
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Sheeja Rajasingh et al.
Acta pharmacologica Sinica, 39(10), 1590-1603 (2018-04-06)
Induced pluripotent stem cell (iPSC)-based cardiac regenerative medicine requires the efficient generation, structural soundness and proper functioning of mature cardiomyocytes, derived from the patient's somatic cells. The most important functional property of cardiomyocytes is the ability to contract. Currently available
Serdar Durdagi et al.
Journal of molecular graphics & modelling, 74, 153-170 (2017-05-13)
The intra-cavitary drug blockade of hERG1 channel has been extensively studied, both experimentally and theoretically. Structurally diverse ligands inadvertently block the hERG1 K
K Lansu et al.
Cell death & disease, 4, e652-e652 (2013-06-08)
Traditionally the hERG1 potassium channel has been known to have a fundamental role in membrane excitability of several mammalian cells including cardiac myocytes. hERG1 has recently been found to be expressed in non-excitable cancer cells of different histogenesis, but the
Global Trade Item Number
| SKU | GTIN |
|---|---|
| N0663-25MG | 04061832574981 |
| N0663-5MG | 04061834092971 |