NNC 55-0396 dihydrochloride

Описание

NNC 55-0396 is a selective inhibitor of T-type calcium channels that blocks Ca_v3.1 in stably expressing HEK293 cells (IC₅₀ = 6.8 μM) with no discernible effect on high voltage-activated (L-type) channels in INS-1 cells up to a concentration of 100 μM. NNC 55-0396 suppresses tremor in two murine models, the GABA_A α₁-null (20 mg/kg) and harmaline-induced (12.5 mg/kg) tremor models, and was better tolerated than mibefradil . In arterial smooth muscle cells, NCC 55-0396 (IC₅₀ = 80 nM) inhibits voltage-dependent K⁺ channels but does not affect their voltage sensitivity. NNC 55-0396 (1-5 μM) also suppresses angiogenesis in vitro by inhibiting hypoxia-inducible factor-1α activity, and it slows tumor growth of flank xenografts of U87MG cells in mice when administered at 20 mg/kg.

Использование

NNC 55-0396 is a calcium channel protein inhibitor.

Биологическая активность

Highly selective T-type calcium channel blocker. Displays IC 50 values of 6.8 and > 100 μ M for inhibition of Cav3.1 T-type channels and HVA currents respectively in INS-1 cells.