Mibefradil dihydrochloride
Based on 14 publication(s) in Google Scholar
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.
- Purity: 99.71%
- CAS No.: 116666-63-8
- Formula: C29H40Cl2FN3O3
- Molecular Weight:568.55
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Storage:
-20°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Mibefradil dihydrochloride
More- ACS Nano. 2024 Nov 12;18(45):31451-31465. [Abstract]
- Neuron. 2026 Mar 27:S0896-6273(26)00126-1. [Abstract]
- Small. 2024 Aug 10:e2403381. [Abstract]
- Br J Pharmacol. 2021 Jan;178(2):346-362. [Abstract]
- PLoS Biol. 2024 Mar 25;22(3):e3002565. [Abstract]
- Front Pharmacol. 2022 Feb 23;13:816133. [Abstract]
- Eur J Pharmacol. 2021 Feb 5;892:173782. [Abstract]
- Mediators Inflamm. 2020 Nov 10;2020:3691701. [Abstract]
- J Cell Physiol. 2021 Sep;236(9):6548-6558. [Abstract]
- Theriogenology. 2021 Jan 1;159:140-146. [Abstract]
- Biochem Biophys Res Commun. 2025 Sep 19:785:152676. [Abstract]
- Biochem Biophys Res Commun. 2020 Feb 19;522(4):862-868. [Abstract]
- Biocell. 2026 Jan 23.
- Res Sq. 2024 Jun 11.
All Calcium Channel Isoforms
More
Biological Activity
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L-type calcium channel |
T-type calcium channel |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
24.6 μM
Compound: 28
|
Inhibition of human TASK3 expressed in HEK293 cells by Ti+ flux assay
Inhibition of human TASK3 expressed in HEK293 cells by Ti+ flux assay
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[PMID: 31260312] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 116666-63-8
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Appearance Solid
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Molecular Weight 568.55
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Formula C29H40Cl2FN3O3
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Color White to yellow
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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
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Synonyms
Ro 40-5967 dihydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
Publications (14)
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Journal Impact Factor
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Most Recent
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ACS Nano
Single-Molecule-Based, Label-Free Monitoring of Molecular Glue Efficacies for Promoting Protein-Protein Interactions Using YaxAB Nanopores. [Abstract]2024 Nov 12;18(45):31451-31465. PMID: 39482865 -
Neuron
Molecular brake on firing pattern transitions in MHbChAT neurons to mediate nicotine-withdrawal-induced anxiety. [Abstract]2026 Mar 27:S0896-6273(26)00126-1. PMID: 41903536 -
Small
2024 Aug 10:e2403381. PMID: 39126240 -
Br J Pharmacol
Small intestinal glucose and sodium absorption through calcium-induced calcium release and store-operated Ca2+ entry mechanisms. [Abstract]2021 Jan;178(2):346-362. PMID: 33080043 -
PLoS Biol
The scale of zebrafish pectoral fin buds is determined by intercellular K+ levels and consequent Ca2+-mediated signaling via retinoic acid regulation of Rcan2 and Kcnk5b. [Abstract]2024 Mar 25;22(3):e3002565. PMID: 38527087 -
Front Pharmacol
Ca2+-Permeable Channels/Ca2+ Signaling in the Regulation of Ileal Na+/Gln Co-Transport in Mice. [Abstract]2022 Feb 23;13:816133. PMID: 35281933 -
Eur J Pharmacol
T-type calcium channels blockers inhibit HSV-2 infection at the late stage of genome replication. [Abstract]2021 Feb 5;892:173782. PMID: 33279521 -
Mediators Inflamm
Mibefradil and Flunarizine, Two T-Type Calcium Channel Inhibitors, Protect Mice against Lipopolysaccharide-Induced Acute Lung Injury. [Abstract]2020 Nov 10;2020:3691701. PMID: 33223955 -
J Cell Physiol
Effects of various calcium transporters on mitochondrial Ca2+ changes and oocyte maturation. [Abstract]2021 Sep;236(9):6548-6558. PMID: 33704771 -
Theriogenology
Lysine acetylation participates in boar spermatozoa motility and acrosome status regulation under different glucose conditions. [Abstract]2021 Jan 1;159:140-146. PMID: 33152539 -
Biochem Biophys Res Commun
Glucose transports in the ileum: mechanism, regulation and physiological role of ileal glucose absorption. [Abstract]2025 Sep 19:785:152676. PMID: 41005286 -
Biochem Biophys Res Commun
Combinatorial screening of a panel of FDA-approved drugs identifies several candidates with anti-Ebola activities. [Abstract]2020 Feb 19;522(4):862-868. PMID: 31806372 -
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Solvent & Solubility
H2O : 150 mg/mL (263.83 mM; Need ultrasonic)
DMSO : 50 mg/mL (87.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, away from moisture). 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.
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, away from moisture). 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
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, away from moisture). 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 |
|---|---|---|---|---|---|
| DMSO / 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 | |
| H2O | 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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