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Mibefradil

Catalog No. TQ0153 CAS 116644-53-2

Synonyms: 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).

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Mibefradil, CAS 116644-53-2

Pack Size	Availability	Price/USD
25 mg	10-14 weeks	$ 2,420.00
50 mg	10-14 weeks	$ 3,180.00
100 mg	10-14 weeks	$ 4,300.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

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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, L-type:18.6 μM, Ca2+ channel, T-type:2.7 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	The hearing thresholds of the 24-26 week old C57BL/6J mice differed 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 [3]. Compared with the saline-treated group, rats receiving Mibefradil show significantly lower CaV3.2 expression in the spinal cord and DRG [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
Molecular Weight	495.63
Formula	C29H38FN3O3
CAS No.	116644-53-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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)

References and Literature

1. Mehrke G, et al. The Ca(++)-channel blocker Ro 40-5967 blocks differently T-type and L-type Ca++ channels. J Pharmacol Exp Ther. 1994 Dec;271(3):1483-8. 2. Brain KL, et al. The sources and sequestration of Ca(2+) contributing to neuroeffector Ca(2+) transients in the mouse vas deferens. J Physiol. 2003 Dec 1;553(Pt 2):627-35. 3. Yu YF, et al. Protection of the cochlear hair cells in adult C57BL/6J mice by T-type calcium channel blockers. Exp Ther Med. 2016 Mar;11(3):1039-1044. 4. Shiue SJ, et al. Chronic intrathecal infusion of T-type calcium channel blockers attenuates CaV3.2 upregulation in nerve-ligated rats. Acta Anaesthesiol Taiwan. 2016 Oct 17. pii: S1875-4597(16)30071-6.

Citations

1. Zhang H, Chen C, Liu Y, et al. NRF-2/HO-1 Pathway-Mediated SHOX2 Activation Is a Key Switch for Heart Rate Acceleration by Yixin-Fumai Granules. Oxidative Medicine and Cellular Longevity. 2022

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Keywords

Mibefradil 116644-53-2 Membrane transporter/Ion channel Metabolism Calcium Channel Ro 40-5967 inhibitor inhibit

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