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Mibefradil

Name: Mibefradil
Brand: TargetMol
SKU: TQ0153
Rating: 4.5 (1 reviews)

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Catalog No. TQ0153Cas No. 116644-53-2

Alias Ro 40-5967

Mibefradil is a calcium channel blocker with moderate selectivity for T-type Ca2+ channels (IC50s: 2.7 μM and 18.6 μM for T-type and L-type currents).

Mibefradil

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Catalog No. TQ0153Alias Ro 40-5967Cas No. 116644-53-2

Mibefradil is a calcium channel blocker with moderate selectivity for T-type Ca2+ channels (IC50s: 2.7 μM and 18.6 μM for T-type and L-type currents).

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$2,420	10-14 weeks	10-14 weeks
50 mg	$3,180	10-14 weeks	10-14 weeks
100 mg	$4,300	10-14 weeks	10-14 weeks

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Product Introduction

Bioactivity

Description	Mibefradil is a calcium channel blocker with moderate selectivity for T-type Ca2+ channels (IC50s: 2.7 μM and 18.6 μM for T-type and L-type currents).
Targets&IC50	Ca2+ channel, T-type:2.7 μM, Ca2+ channel, L-type:18.6 μM
In vitro	Mibefradil (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 %) and causes a significant membrane potential depolarization (from ?83±1 mV to ?71±5 mV). At a higher Mibefradil concentration (20 μM) there is significant membrane potential depolarization and a slowing of repolarization [2].
In vivo	After the 4-week treatment period, the hearing thresholds of 24-26-week-old C57BL/6J mice varied. The threshold at 24 kHz significantly decreased in the Mibefradil-treated and benidipine-treated groups compared to the saline-treated group [3]. Additionally, rats treated with Mibefradil displayed markedly lower CaV3.2 expression in the spinal cord and DRG than the saline-treated group [4].
Animal Research	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 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 a 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 [3]. 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 Ethosuximide (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 [4].
Synonyms	Ro 40-5967

Chemical Properties

Molecular Weight	495.63
Formula	C₂₉H₃₈FN₃O₃
Cas No.	116644-53-2
Smiles	C(CN(CCCC=1NC=2C(N1)=CC=CC2)C)[C@]3(OC(COC)=O)[C@@H]([C@@H](C)C)C=4C(CC3)=CC(F)=CC4
Relative Density.	1.18g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: 95 mg/mL (191.68 mM), Heating is recommended.

Ethanol: 52 mg/mL (104.92 mM), Heating is recommended.

DMSO: 50 mg/mL (100.88 mM), Sonication is recommended.

Solution Preparation Table

DMSO/Ethanol/H2O

	1mg	5mg	10mg	50mg
1 mM	2.0176 mL	10.0882 mL	20.1763 mL	100.8817 mL
5 mM	0.4035 mL	2.0176 mL	4.0353 mL	20.1763 mL
10 mM	0.2018 mL	1.0088 mL	2.0176 mL	10.0882 mL
20 mM	0.1009 mL	0.5044 mL	1.0088 mL	5.0441 mL
50 mM	0.0404 mL	0.2018 mL	0.4035 mL	2.0176 mL
100 mM	0.0202 mL	0.1009 mL	0.2018 mL	1.0088 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc