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N0663

Sigma-Aldrich

NS1643

≥98% (HPLC), solid

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About This Item

Empirische Formel (Hill-System):
C15H10F6N2O3
CAS-Nummer:
448895-37-2
Molekulargewicht:
380.24
MDL-Nummer:
MFCD08705418
UNSPSC-Code:
12352200
PubChem Substanz-ID:
24897438
NACRES:
NA.77

Qualitätsniveau

100

Assay

≥98% (HPLC)

Form

solid

Farbe

white to off-white

Löslichkeit

DMSO: ≥20 mg/mL

Lagertemp.

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)

InChIKey

NJFVQMRYJZHGME-UHFFFAOYSA-N

Biochem./physiol. Wirkung

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.

Leistungsmerkmale und Vorteile

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.

Piktogramme

Skull and crossbones
GHS06

Signalwort

Danger

H-Sätze

H301 - H319

Gefahreneinstufungen

Acute Tox. 3 Oral - Eye Irrit. 2

Lagerklassenschlüssel

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

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Persönliche Schutzausrüstung

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

Analysenzertifikate (COA)

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Die Dokumentenbibliothek aufrufen

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
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
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
H R Lu et al.
Journal of pharmacological and toxicological methods, 87, 53-67 (2017-05-16)
Human induced pluripotent stem cell-derived cardiomyocytes (hiPS-CMs) are emerging as new and human-relevant source in vitro model for cardiac safety assessment that allow us to investigate a set of 20 reference drugs for predicting cardiac arrhythmogenic liability using optical action
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