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Mibefradil  ≥98%

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包装规格：10mg in glass bottle
产品描述：基本信息 产品编号： M11264 产品名称： Mibefradil CAS: 116644-53-2   储存条件 粉末 -20℃ 四年 分子式： C29H38FN3O3 溶于液体 -80℃ 一年 分子量： 495.63     化学名：  Acetic acid,methoxy-,(1S,2S)-2-[2-[[3-(1H-benzimidazol-2-yl)propyl]methylamino]ethyl]-6-fluoro-1,2,3,4-tetrahydro-1-(1-methylethyl)-2-naphthalenyl ester Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   生物活性 产品描述 一种钙离子通道(calciumchannel)阻断剂 靶点 IC50: 2.7μM (T-type calcium channel),18.6μM (L-type calcium channel)   体外研究 Mibefradil inhibits reversibly the T-and L-type currents with IC50 values of 2.7 and 18.6μM,respectively.The inhibition of the L-type current is voltage-dependent,whereas that of the T-type current is not.Ro 40-5967 blocks T-type current already at a holding potential of -100 mV At a higher concentration (20µM),Mibefradil reduces the amplitude of excitatory junction potentials (by 37±10 %),slows the rate of repolarisation (by 44±16 %) and causes a significant membrane potential depolarisation (from −83±1 mV to −71±5 mV).At a higher Mibefradil concentration (20µM) there is significant membrane potential depolarisation and a slowing of repolarisation.These actions of Mibefradil are consistent with K+ channel inhibition,which has been shown to occur in human myoblasts and other cells. 体内研究 The hearing thresholds of the 24-26 week old C57BL/6J mice differed following the 4-week treatment period.The hearing threshold at 24 kHz is significantly decreased in the Mibefradil-treated and benidipine-treated groups compared with the saline-treated group (P<0.05).Compared with the saline-treated group,rats receiving Mibefradil or Ethosuximide show significant lower CaV3.2 expression in the spinal cord and DRG.   推荐实验方法(仅供参考) 动物实验:   Mice A total of 30 male C57BL/6J mice (age,6-8 weeks) are randomized into three groups for the detection of three calcium channel receptor subunits α1G,α1H andα1I,using reverse transcription-quantitative polymerase chain reaction (RT-qPCR).In addition, a further 30 C57BL/6J male mice (age,24-26 weeks) are allocated at random into three treatment groups:Saline,Mibefradil and benidipine.Each group is subjected to auditory brainstem recording (ABR) and distortion product otoacoustic emission (DPOAE) tests following treatment.Mibefradil and benidipine are dissolved in physiological saline solution.A preliminary experiment led to the selection of dosages of 30mg/kg/day Mibefradil and 10mg/kg/day Benidipine.The drugs are administered to the mice by gavage for four consecutive weeks. Rats Male Sprague-Dawley rats (200-250 g) are used for right L5/6 SNL to induce neuropathic pain. Intrathecal infusion of saline or TCC blockers [Mibefradil (0.7μg/h) or Ethosuximide (60 μg/h)] is started after surgery for 7 days. Fluorescent immunohistochemistry and Western blotting are used to determine the expression pattern and protein level of CaV3.2.Hematoxylin-eosin and toluidine blue staining are used to evaluate the neurotoxicity of tested agents.
保存条件：-20℃

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