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

Mibefradil dihydrochloride (Synonyms: Ro 40-5967 dihydrochloride)

Cat. No.: HY-15553A Purity: 98.78%
Handling Instructions

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).

For research use only. We do not sell to patients.

Mibefradil dihydrochloride Chemical Structure

Mibefradil dihydrochloride Chemical Structure

CAS No. : 116666-63-8

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10 mM * 1 mL in Water USD 128 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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10 mg USD 182 In-stock
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50 mg USD 802 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

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Description

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

IC50: 2.7 μM (T-type calcium channel), 18.6 μM (L-type calcium channel)[1]

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[1] 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[2].

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

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)[3]. Compared with the saline-treated group, rats receiving Mibefradil or NSC 64013 show significant lower CaV3.2 expression in the spinal cord and DRG[4].

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

Clinical Trial
Molecular Weight

568.55

Formula

C₂₉H₄₀Cl₂FN₃O₃

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

H2O : ≥ 125 mg/mL (219.86 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
References
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.

References

Purity: 98.78%

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Mibefradil dihydrochloride
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