| 货号 | 17216-1mg |
| 描述 | NNC 55-0396 is a selective inhibitor of T-type calcium channels that blocks Cav3.1 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.1 NNC 55-0396 suppresses tremor in two murine models, the GABAAα1-null (20 mg/kg) and harmaline-induced (12.5 mg/kg) tremor models, and was better tolerated than mibefradil (Item No. 15037).2 In arterial smooth muscle cells, NCC 55-0396 (IC50 = 80 nM) inhibits voltage-dependent K+ channels but does not affect their voltage sensitivity.3 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.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Huang, L.,Keyser, B.M.,Tagmose, T.M., et al. NNC 55-0396 [(1S,2S)-2-(2-(N-[(3-benzimidazol-2-yl)propyl]-N-methylamino)ethyl)-6-fluoro-1,2,3,4-tetrahydro-1-isopropyl-2-naphtyl cyclopropanecarboxylate dihydrochloride]: a new selective inhibitor of T-type calcium channels. J. Pharmacol. Exp. Ther. 309(1), 193-199 (2004). 2.Quesada, A.,Bui, P.H.,Homanics, G.E., et al. Comparison of mibefradil and derivative NNC 55-0396 effects on behavior, cytochrome P450 activity, and tremor in mouse models of essential tremor. Eur. J. Pharmacol. 659(1), 30-36 (2011). 3.Son, Y.K.,Hong, D.H.,Li, H., et al. Ca2+ channel inhibitor NNC 55-0396 inhibits voltage-dependent K+ channels in rabbit coronary arterial smooth muscle cells. J. Pharmacol. Sci. 125(3), 312-319 (2014). 4.Kim, K.H.,Kim, D.,Park, J.Y., et al. NNC 55-0396, a T-type Ca2+ channel inhibitor, inhibits angiogenesis via suppression of hypoxia-inducible factor-1α signal transduction. J. Mol. Med. (Berlin) 93(5), 499-509 (2015). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 564.6 |
| 分子式 | C30H38FN3O2 • 2HCl |
| CAS号 | 357400-13-6 |
| 稳定性 | ≥ 2 years |
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