1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. Calcium Channel
  3. Mibefradil dihydrochloride

Mibefradil dihydrochloride  (Synonyms: 盐酸米贝地尔; Ro 40-5967 dihydrochloride)

目录号: HY-15553A 纯度: ≥98.0%
COA 产品使用指南

Mibefradil dihydrochloride (Ro 40-5967 dihydrochloride) 是一种钙离子通道 (calcium channel) 抑制剂,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。

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Mibefradil dihydrochloride Chemical Structure

Mibefradil dihydrochloride Chemical Structure

CAS No. : 116666-63-8

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Mibefradil dihydrochloride (Ro 40-5967 dihydrochloride) is a calcium channel blocker with moderate selectivity for T-type Ca2+ channels (IC50s of 2.7 μM and 18.6 μM for T-type and L-type currents, respectively)[1].

IC50 & Target

L-type calcium channel

 

T-type calcium channel

 

体外研究
(In Vitro)

Mibefradil dihydrochloride 可逆地抑制 T 型和 L 型电流,IC50 值分别为 2.7 和 18.6 μM。L 型电流的抑制是电压依赖性的,而 T 型电流的抑制不是。Ro 40-5967 阻断 T 型电流已经处于-100 mV 的保持电位[1]。在较高浓度 (20 μM) 下,Mibefradil 降低了兴奋性结电位的幅度 (37±10 %),减慢复极化速率 (44±16%) 并导致显著的膜电位去极化 (从-83±1 mV 到-71±5 mV)。在较高的 Mibefradil dihydrochloride 浓度 (20 μM) 下,存在显著的膜电位去极化和复极化减慢。Mibefradil 的这些作用与 K+ 通道抑制一致,K+ 通道抑制已被证明发生在人成肌细胞和其他细胞中[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

24-26 周大的 C57BL/6J 小鼠的听力阈值在 4 周的处理期后有所不同。与生理盐水处理组相比,Mibefradil dihydrochloride 处理组和贝尼地平处理组的 24 kHz 听阈显著降低 (P<0.05)[3]。与生理盐水组相比,Mibefradil dihydrochloride 或 NSC 64013 组大鼠脊髓和 DRG中 CaV3.2 表达显著降低[4]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

568.55

Formula

C29H40Cl2FN3O3

CAS 号
性状

固体

颜色

White to yellow

中文名称

盐酸米贝拉地尔;盐酸米贝地尔;盐酸咪拉地尔;盐酸咪贝地尔

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
In Vitro: 

H2O 中的溶解度 : 150 mg/mL (263.83 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7589 mL 8.7943 mL 17.5886 mL
5 mM 0.3518 mL 1.7589 mL 3.5177 mL
查看完整储备液配制表

* 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
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料
参考文献
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 NSC 64013 (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 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

Mibefradil dihydrochloride 相关分类

完整储备液配制表

* 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
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 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
15 mM 0.1173 mL 0.5863 mL 1.1726 mL 2.9314 mL
20 mM 0.0879 mL 0.4397 mL 0.8794 mL 2.1986 mL
25 mM 0.0704 mL 0.3518 mL 0.7035 mL 1.7589 mL
30 mM 0.0586 mL 0.2931 mL 0.5863 mL 1.4657 mL
40 mM 0.0440 mL 0.2199 mL 0.4397 mL 1.0993 mL
50 mM 0.0352 mL 0.1759 mL 0.3518 mL 0.8794 mL
60 mM 0.0293 mL 0.1466 mL 0.2931 mL 0.7329 mL
80 mM 0.0220 mL 0.1099 mL 0.2199 mL 0.5496 mL
100 mM 0.0176 mL 0.0879 mL 0.1759 mL 0.4397 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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