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Mibefradil dihydrochloride

Mibefradil dihydrochloride

产品编号 T12032   CAS 116666-63-8
别名: 盐酸米贝地尔, Ro 40-5967 (dihydrochloride), 米贝拉地尔

Mibefradil dihydrochloride (Ro 40-5967 (dihydrochloride)) 是一种钙离子通道抑制剂,选择性作用于 T 型 Ca2+通道,对 T 型和 L 型通道的IC50分别为 2.7 和 18.6 μM。

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Mibefradil dihydrochloride Chemical Structure
Mibefradil dihydrochloride, CAS 116666-63-8
规格 价格/CNY 货期 数量
1 mg ¥ 278 现货
5 mg ¥ 713 现货
其他形式的 Mibefradil dihydrochloride:
产品目录号及名称: Mibefradil dihydrochloride (T12032)
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选择批次  
纯度: 99.72%
纯度: 99.72%
纯度: 99.45%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Mibefradil dihydrochloride (Ro 40-5967 (dihydrochloride)) is an blocker of calcium channel with moderate selectivity for T-type Ca2+ channels (T-type and L-type currents with IC50s of 2.7 μM and 18.6 μM, respectively).
靶点活性 L-type calcium channel:18.6 μM , T-type calcium channel:2.7 μM
体外活性 Mibefradil dihydrochloride inhibits reversibly the T- and L-type currents with IC50 values of 2.7 and 18.6 μM, respectively.[1].Mibefradil inhibited Orai1, Orai2, and Orai3 currents dose-dependently. The IC50 for Orai1, Orai2, and Orai3 channels was 52.6, 14.1, and 3.8 μM respectively. Outside-out patch demonstrated that perfusion of 10-μM mibefradil to the extracellular surface completely blocked Orai3 currents and single channel activity evoked by 2-APB. Intracellular application of mibefradil did not alter Orai3 channel activity. Mibefradil at higher concentrations (>50 μM) inhibited Ca2+ release but had no effect on cytosolic STIM1 translocation evoked by thapsigargin. Inhibition on Orai channels by mibefradil was structure-related, as other T-type Ca2+ channel blockers with different structures, such as ethosuximide and ML218, had no or minimal effects on Orai channels. Moreover, mibefradil inhibited cell proliferation, induced apoptosis, and arrested cell cycle progression[3].
体内活性 Compared with the saline-treated group, rats receiving Mibefradil or Ethosuximide show significant lower CaV3.2 expression in the spinal cord and DRG.
细胞实验 Human Orai1-3 cDNAs in tetracycline-regulated pcDNA4/TO vectors were transfected into HEK293 T-REx cells with stromal interaction molecule 1 (STIM1) stable expression. The Orai currents were recorded by whole-cell and excised-membrane patch clamp. Ca2+?influx or release was measured by Fura-PE3/AM. Cell growth and death were monitored by WST-1, LDH assays and flow cytometry[3].
别名 盐酸米贝地尔, Ro 40-5967 (dihydrochloride), 米贝拉地尔
分子量 568.55
分子式 C29H40Cl2FN3O3
CAS No. 116666-63-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: 122 mg/mL (214.58mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 1.7589 mL 8.7943 mL 17.5886 mL 43.9715 mL
5 mM 0.3518 mL 1.7589 mL 3.5177 mL 8.7943 mL
10 mM 0.1759 mL 0.8794 mL 1.7589 mL 4.3972 mL
20 mM 0.0879 mL 0.4397 mL 0.8794 mL 2.1986 mL
50 mM 0.0352 mL 0.1759 mL 0.3518 mL 0.8794 mL
100 mM 0.0176 mL 0.0879 mL 0.1759 mL 0.4397 mL

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
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. 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. 2. 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. 3. Li P , Rubaiy H N , Gui‐Lan Chen, et al. Mibefradil, a T‐type Ca2+ channel blocker also blocks Orai channels by action at the extracellular surface[J]. British Journal of Pharmacology, 2019, 176. 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.
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相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 抗癌药物库 经典已知活性库 抗心血管疾病化合物库 抗癌化合物库 钙通道分子库 抗高血压化合物库 临床期小分子药物库 NO PAINS 化合物库 代谢化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

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: 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 μL,一共给药动物10 只,您使用的配方为5% 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 μL DMSO (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:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步: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
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Mibefradil dihydrochloride 116666-63-8 Membrane transporter/Ion channel Metabolism Calcium Channel inhibit 盐酸米贝地尔 Mibefradil Dihydrochloride Ro 40-5967 (dihydrochloride) Inhibitor Ca channels Ca2+ channels 米贝拉地尔 Mibefradil Ro 40-5967 inhibitor

 

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