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

Mibefradil dihydrochloride  (Synonyms: Ro 40-5967 dihydrochloride)

Cat. No.: HY-15553A Purity: ≥98.0%
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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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Solid + Solvent
10 mM * 1 mL in Water
ready for reconstitution
 USD 141 In-stock
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Based on 9 publication(s) in Google Scholar

Other Forms of Mibefradil dihydrochloride:

Mibefradil dihydrochloride Related Antibodies

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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

L-type calcium channel

 

T-type 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[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].

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

Mibefradil dihydrochloride Related Antibodies
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].

MedChemExpress (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.
Appearance

Solid

Color

White to yellow

SMILES

O=C(O[C@@]1(CCN(CCCC2=NC3=CC=CC=C3N2)C)[C@@H](C(C)C)C4=C(C=C(F)C=C4)CC1)COC.[H]Cl.[H]Cl
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 : 150 mg/mL (263.83 mM; Need ultrasonic)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Mibefradil dihydrochloride Related Classifications

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  • 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.

Keywords:

Mibefradil116666-63-8Ro 40-5967Calcium ChannelCa2+ channelsCa channelsInhibitorinhibitorinhibit

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