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Mibefradil

MCE 国际站：Mibefradil

品牌：MedChemExpress (MCE)

货号：HY-15553

CAS 号：116644-53-2

生物活性：米贝地尔（Ro 40-5967）是一种钙通道阻滞剂，对 T 型 Ca2+ 通道具有中等选择性，对 T 型和 L 型电流的 IC50 分别为 2.7 μM 和 18.6 μM[1]。

体外研究(In Vitro)：Mibefradil inhibits reversibly the T- and L-type currents with IC50 values of 2.7 and 18.6 μM, 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[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±16 %) and causes a significant membrane potential depolarisation (from 83±1 mV to 71±5 mV). At a higher Mibefradil concentration (20 μM) 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[2]. MCE尚未独立确认这些方法的准确性。 仅供参考。

体内研究(In Vivo)：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[3]. Compared with the saline-treated group, rats receiving Mibefradil or Ethosuximide show significant lower CaV3.2 expression in the spinal cord and DRG[4]. MCE尚未独立确认这些方法的准确性。 仅供参考。

分子量：495.63

Formula：C29H38FN3O3

性状：固体

颜色：White to off-white

中文名称：米贝拉地尔；米贝地尔；咪拉地尔；咪贝地尔

运输条件：美国大陆地区的室温；其他地区可能有所不同。

储存方式：-20°C，密封保存，避光防潮 *溶剂保存：-80°C，6个月；-20°C，1个月（密封保存，避光防潮）

Animal Administration [3][4]：Mice[3] 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 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 30 mg/kg/day Mibefradil and 10 mg/kg/day Benidipine. The drugs are administered to the mice by gavage for four consecutive weeks. Rats[4] 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. MCE尚未独立确认这些方法的准确性。 仅供参考。

文献引用：MCE 顾客使用本产品发表 14 篇科研文献

提供质量检测报告：Data Sheet、产品使用指南

产品活性：Mibefradil (Ro 40-5967) 是一种钙离子通道 (calcium channel) 阻断剂，选择性作用于 T 型 Ca2+通道，作用于 T 型和 L 型通道，IC50 分别为 2.7 μM 和 18.6 μM。

IC50 & Target：L-type calcium channel

相关产品：Mibefradil dihydrochloride  | (S)-(-)-Bay-K-8644  | (R)-(+)-Bay-K-8644  | SG-094  | S107  | JTV-519 hemifumarate  | TMDJ-035  | MK-7622  | Calcium Channel antagonist 2  | D-myo-Inositol 1,4,5-trisphosphate tripotassium  | Thio-NADP  | NAADP tetrasodium

热门产品线：抑制剂  | 稳定性同位素标记物  |  脂质  |  糖类

Trending products：Inhibitors  | Isotope-Labeled Compounds  |  Lipids  |  Saccharides

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客户发表文献：
[1]. Nature. 2026 Sep;657(8131):549-558.
[2]. Nature. 2026 Sep;657(8132):755-764.
[3]. Nature. 2026 Sep;657(8133):1027-1034.
[4]. Nature. 2026 Sep;657(8131):477-486.
[5].Nature. 2026 Sep;657(8132):789-799.
[6]. Nature. 2026 Sep;657(8131):517-524.
[7]. Nature. 2026 Sep;657(8133):1045-1052.
[8]. Cell. 2026 Sep 14:S0092-8674(26)01003-2.
[9]. Cell. 2026 Sep 3;189(18):5688-5705.e13.
[10]. Cell. 2026 Sep 2:S0092-8674(26)00937-2.

参考文献：
[1]. Mehrke G, et al. The Ca(++)-channel blocker Ro 40-5967 blocks differently T-type and L-type Ca++ channels. J Pharmacol Exp Ther. 1994 Dec;271(3):1483-8.
[2]. Brain KL, et al. The sources and sequestration of Ca(2+) contributing to neuroeffector Ca(2+) transients in the mouse vas deferens. J Physiol. 2003 Dec 1;553(Pt 2):627-35.
[3]. Yu YF, et al. Protection of the cochlear hair cells in adult C57BL/6J mice by T-type calcium channel blockers. Exp Ther Med. 2016 Mar;11(3):1039-1044.
[4]. Shiue SJ, et al. Chronic intrathecal infusion of T-type calcium channel blockers attenuates CaV3.2 upregulation in nerve-ligated rats. Acta Anaesthesiol Taiwan. 2016 Oct 17. pii: S1875-4597(16)30071-6.