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NNC 55-0396
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
NNC 55-0396图片
CAS NO:357400-13-6
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
NNC 55-0396，Mibefradil 衍生物，是一种高选择性的 T 型钙通道阻滞剂；显示 6.8 和 >100 μM 的 IC50 值分别抑制 INS-1 细胞中的 Cav3.1 T 型通道和 HVA 电流。
Cas No.357400-13-6
别名NNC 55-0396 dihydrochloride
化学名2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)(methyl)amino)ethyl)-6-fluoro-1-isopropyl-1,2,3,4-tetrahydronaphthalen-2-yl cyclopropanecarboxylate dihydrochloride
Canonical SMILESCC(C1C2=C(C=C(F)C=C2)CCC1(OC(C3CC3)=O)CCN(CCCC4=NC5=CC=CC=C5N4)C)C.Cl.Cl
分子式C30H40Cl2FN3O2
分子量564.56
溶解度30mg/mL in ethanol, or in DMSO, in DMF
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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 GABAA α1-null (20 mg/kg) and harmaline-induced (12.5 mg/kg) tremor models, and was better tolerated than mibefradil.[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]

Reference:
[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).