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Mibefradil

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产品编号 TQ0153Cas号 116644-53-2
别名 米贝地尔, Ro 40-5967

Mibefradil is a calcium channel blocker with moderate selectivity for T-type Ca2+ channels (IC50s: 2.7 μM and 18.6 μM for T-type and L-type currents).

Mibefradil

Mibefradil

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产品编号 TQ0153 别名 米贝地尔, Ro 40-5967Cas号 116644-53-2

Mibefradil is a calcium channel blocker with moderate selectivity for T-type Ca2+ channels (IC50s: 2.7 μM and 18.6 μM for T-type and L-type currents).

规格价格库存数量
25 mg
¥ 17,200
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50 mg
¥ 22,800
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100 mg
¥ 29,500
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产品介绍

生物活性
产品描述
Mibefradil is a calcium channel blocker with moderate selectivity for T-type Ca2+ channels (IC50s: 2.7 μM and 18.6 μM for T-type and L-type currents).
靶点活性
Ca2+ channel, L-type:18.6 μM, Ca2+ channel, T-type:2.7 μM
体外活性
Mibefradil (Ro 40-5967) blocks T-type current already at a holding potential of -100 mV [1]. At a higher concentration (20 μM), Mibefradil reduces the amplitude of excitatory junction potentials (by 37±10 %), slows the rate of repolarisation (by 44 %) and causes a significant membrane potential depolarization (from ?83±1 mV to ?71±5 mV). At a higher Mibefradil concentration (20 μM) there is significant membrane potential depolarization and a slowing of repolarization [2].
体内活性
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 [3]. Compared with the saline-treated group, rats receiving Mibefradil show significantly lower CaV3.2 expression in the spinal cord and DRG [4].
动物实验
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 and α1I, using 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 a physiological saline solution. A preliminary experiment led to the selection of dosages of 30 mg/kg/day Mibefradil and 10 mg/kg/day Benidipine. The drugs are administered to the mice by gavage for four consecutive weeks [3]. 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 (0.7 μg/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 [4].
别名米贝地尔, Ro 40-5967
化学信息
分子量495.63
分子式C29H38FN3O3
CAS No.116644-53-2
密度1.18g/cm3
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
H2O: 95 mg/mL (191.68 mM), Heating is recommended.
Ethanol: 52 mg/mL (104.92 mM), Heating is recommended.
DMSO: 50 mg/mL (100.88 mM), Sonication is recommended.
溶液配制表
DMSO/Ethanol/H2O
1mg5mg10mg50mg
1 mM2.0176 mL10.0882 mL20.1763 mL100.8817 mL
5 mM0.4035 mL2.0176 mL4.0353 mL20.1763 mL
10 mM0.2018 mL1.0088 mL2.0176 mL10.0882 mL
20 mM0.1009 mL0.5044 mL1.0088 mL5.0441 mL
50 mM0.0404 mL0.2018 mL0.4035 mL2.0176 mL
100 mM0.0202 mL0.1009 mL0.2018 mL1.0088 mL

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计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
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μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

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