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N0663

Sigma-Aldrich

NS1643

≥98% (HPLC), solid

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About This Item

Fórmula empírica (notación de Hill):
C15H10F6N2O3
Número de CAS:
448895-37-2
Peso molecular:
380.24
Número MDL:
MFCD08705418
Código UNSPSC:
12352200
ID de la sustancia en PubChem:
24897438
NACRES:
NA.77

Nivel de calidad

100

Ensayo

≥98% (HPLC)

Formulario

solid

color

white to off-white

solubilidad

DMSO: ≥20 mg/mL

temp. de almacenamiento

2-8°C

cadena SMILES

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)

Clave InChI

NJFVQMRYJZHGME-UHFFFAOYSA-N

Acciones bioquímicas o fisiológicas

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.

Características y beneficios

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.

Pictogramas

Skull and crossbones
GHS06

Palabra de señalización

Danger

Frases de peligro

H301,H319

Clasificaciones de peligro

Acute Tox. 3 Oral - Eye Irrit. 2

Código de clase de almacenamiento

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable

Equipo de protección personal

dust mask type N95 (US), Eyeshields, Faceshields, Gloves

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Certificados de análisis (COA)

Lot/Batch Number
023M4606V
076K4610

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Visite la Librería de documentos

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
Eun-Kyoung Breuer et al.
Cell death & disease, 10(3), 180-180 (2019-02-23)
Potassium ion channels are critical in the regulation of cell motility. The acquisition of cell motility is an essential parameter of cancer metastasis. However, the role of K+ channels in cancer metastasis has been poorly studied. High expression of the
Jacqueline A Treat et al.
Biochemical pharmacology, 169, 113608-113608 (2019-08-30)
Human induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs) are used for many applications including safety pharmacology. However, a deficiency or complete absence of several K+ currents suggests repolarization reserve is low in hiPSC-CMs. We determined whether a dual Ito and IKr
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