Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 278 | 现货 | ||
5 mg | ¥ 713 | 现货 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 122 mg/mL (214.58mM)
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
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