F15845

Names

[ Name ]:
F15845

[Synonym ]:
UNII-937TSH5BGH
3-(R)-((3-((2-Methoxyphenyl)thio)-2-(S)-methylpropyl)amino)-3,4-dihydro-2H-1,5-benzoxathiepin
(3R)-N-((2S)-3-((2-Methoxyphenyl)sulfanyl)-2-methylpropyl)-3,4-dihydro-2H-1,5-benzoxathiepin-3-amine
2H-1,5-Benzoxathiepin-3-amine,3,4-dihydro-N-((2S)-3-((2-methoxyphenyl)thio)-2-methylpropyl)-,(3R)

Biological Activity

[Description]:

F 15845 is a highly effective persistent sodium current blocker. F 15845 also is a cardioprotective agent, has anti-ischemic activity and exerts short- and long-term cardioprotection after myocardial infarction. F 15845 can be used for the research of myocardium functional impairment[1].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Sodium Channel

Research Areas >> Cardiovascular Disease

[In Vitro]

F 15845 (10 nM-10 μM) concentration-dependently reduces veratrine-induced diastolic contracture with an IC50 value of 0.14 μM in isolated atria[1]. F 15845 (0.1-10 μM) preserves viability in isolated cardiomyocytes exposed to lysophosphatidylcholine (LPC)[1]. F 15845 (0.3 μM) significantly counteracts [Na+] increase during no-flow ischemia[1]. F 15845 (0.3 μM, 0-35 min) delays the reduction in [Na+], but marks and maintains upon reperfusion[1].

[In Vivo]

F 15845 (i.v.; 5 mg/kg) exhibits remarkable cardioprotective properties in anesthetized rat[1]. Animal Model: Rat[1] Dosage: 2.5 mg/kg, 5 mg/kg Administration: intravenously Result: Significantly reduced infarct size, decreased of troponin I levels and limited the long-term expansion of infarct size.

[References]

[1]. Bruno Vié, et al. 3-(R)-[3-(2-methoxyphenylthio-2-(S)-methylpropyl]amino-3,4-dihydro-2H-1,5-benzoxathiepine bromhydrate (F 15845) prevents ischemia-induced heart remodeling by reduction of the intracellular Na+ overload. J Pharmacol Exp Ther. 2009 Sep;330(3):696-703.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₀H₂₅NO₂S₂

[ Molecular Weight ]:
375.54800

[ Exact Mass ]:
375.13300

[ PSA ]:
81.09000

[ LogP ]:
4.95720