GS-462808
GS-462808 is an oral active late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with the IC50 of 1.33 μM. GS-462808 can be used for study of arrhythmia.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 1354198-41-6
- Formel: C17H12F3N5O3
- Molecular Weight:391.30
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
IC50 & Target
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Nav1.5 1.33 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
1.9 μM
Compound: 3
|
Inhibition of 0.1 Hz stimulated human Nav1.5alpha expressed in HEK293 cells assessed as inhibition of late sodium current with 3 compound additions for 7 to 8 mins at holding potential -120 mV in presence of late sodium current activator tefluthrin/ATX2 m
Inhibition of 0.1 Hz stimulated human Nav1.5alpha expressed in HEK293 cells assessed as inhibition of late sodium current with 3 compound additions for 7 to 8 mins at holding potential -120 mV in presence of late sodium current activator tefluthrin/ATX2 m
|
[PMID: 27038498] |
Chemical Information
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CAS. Nr. 1354198-41-6
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Molecular Weight 391.30
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Formel C17H12F3N5O3
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SMILES
O=C1N(CC2=NC(C)=NO2)N=C3C=CC(C4=CC=C(OC(F)(F)F)C=C4)=CN31
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Cardiac voltage-sensitive optical mapping
Cardiac voltage-sensitive optical mapping records changes in transmembrane potential from cardiac tissue by staining the preparation with a voltage-sensitive dye and imaging fluorescence changes during electrical activation; the resulting optical action potentials can be used to map activation time, action potential duration, conduction velocity, wavefront propagation, and arrhythmia dynamics. The optical signal represents a relative fluorescence change from a tissue volume rather than a single-cell intracellular recording, so spatial resolution, sampling rate, voltage resolution, optical magnification, light penetration, and motion control must be considered together when interpreting optical action potentials.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)