Mibefradil dihydrochloride (Synonyms:盐酸米贝地尔; Ro 40-5967 dihydrochloride)
目录号 : KM8774 CAS No. : 116666-63-8 纯度 : 98%

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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生物活性

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

体外研究

Mibefradil dihydrochloride 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 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.

体内研究

The hearing thresholds of the 24-26 week old C57BL/6J mice differ 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<0.05). Compared with the saline-treated group, rats receiving Mibefradil or NSC 64013 show significant lower CaV3.2 expression in the spinal cord and DRG.

分子式
C29H40Cl2FN3O3
分子量
568.55
CAS号
116666-63-8
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 : ≥ 125 mg/mL (219.86 mM)

* "≥" means soluble, but saturation unknown.

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
10 mM 0.1759 mL 0.8794 mL 1.7589 mL
*

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。

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科研文献
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