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- 技术资料
- 保存条件:
-20°C, stored under nitrogen
- 英文名:
Ro 40-5967 dihydrochloride
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
116666-63-8
- 规格:
10 mM * 1 mL/1 mg/5 mg/10 mg/50 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥1063.0 |
|---|---|---|---|
| 规格: | 1 mg | 产品价格: | ¥340.0 |
| 规格: | 5 mg | 产品价格: | ¥850.0 |
| 规格: | 10 mg | 产品价格: | ¥1414.0 |
| 规格: | 50 mg | 产品价格: | ¥6212.0 |
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Mibefradil dihydrochloride
CAS No. : 116666-63-8
MCE 国际站:Mibefradil dihydrochloride
产品活性: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。
研究领域:Membrane Transporter/Ion Channel | Neuronal Signaling
作用靶点:Calcium Channel
In Vitro: 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.
In Vivo: 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.
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