GS967

Hersteller MedChem Express
Kategorie Produkte / Inhibitors
Typ Inhibitors
Specific against other
Clon N/A
Menge 10mg
ArtNr HY-12593-10mg
Eclass 6.1 30220300
Eclass 9.0 32160605
Lieferbar
Synonyms
GS-967
CAS No.
1262618-39-2
Purity
>98%
MW
3472153
Formula
C14H7F6N3O
Solubility
10 mM in DMSO
Biological Description
GS967 (GS-458967) is a potent, and selective inhibitor of cardiac late sodium current (late INa ) with IC50 values of 0.13 and 0.21 uM for ventricular myocytes and isolated hearts, respectively.
IC50 & Target: IC50: 0.13 uM (late INa , ventricular myocytes )and 0.21 uM (late INa , isolated hearts)[1]
In Vitro: GS967 (10, 100, 300 nM) completely attenuates the effect of ATX-II (10 nM) to increase action potential duration (APD) and APD variability in ventricular myocytes, with an apparent IC50 value of ?10 nM and decreased the beat-to-beat variability of APD[1].
In Vivo: GS967 prevents and reverses proarrhythmic effects of the late INa enhancer ATX-II and the IKr inhibitor E-4031. GS967 significantly attenuates the proarrhythmic effects of methoxamine 1 clofilium and suppressed ischemia-induced arrhythmias[1]. GS967 causes a reduction of INaP in a frequency-dependent manner, consistent with use-dependent block (UDB). GS967 evokes more potent UDB of INaP (IC50=0.07 uM) than ranolazine (16 uM) and lidocaine (17 uM). GS967 is found to exert these same effects on a prototypical long QT syndromemutation (delKPQ)[2]. GS967 prevents ischemia-induced increases in alternans in the left atrium and left ventricle. GS967 reduces ischemia-induced increases in depolarization heterogeneity and repolarizationheterogeneity. GS967 does not alter heart rate, arterial blood pressure, PR and QT intervals, or QRS duration, but it mildly decreased contractility during ischemia, which was consistent with late INa inhibition[3].
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Available in quantities of 0, 5mg-1mg. Three different samples per customer per year!
Menge: 10mg
Lieferbar: In stock
Listenpreis: 225,71 €
Preis: 225,71 €
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