Cat. No.: HY-15553

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Mibefradil

Name: Mibefradil
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SKU: HY-15553
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(Synonyms: Ro 40-5967)

15 Cited Publications

Customer Review

Based on 15 publication(s) in Google Scholar

Mibefradil (Ro 40-5967) is a calcium channel blocker with moderate selectivity for T-type Ca²⁺ channels displaying IC₅₀s of 2.7 μM and 18.6 μM for T-type and L-type currents, respectively.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Mibefradil dihydrochloride) that retains the same biological activity.

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

CAS No.: 116644-53-2
Formula: C₂₉H₃₈FN₃O₃
Molecular Weight:495.63

Storage:

-20°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Data Sheet (275 KB)

Mibefradil Chemical Structure

CAS No.: 116644-53-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (15)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

L-type calcium channel

T-type calcium channel

All Calcium Channel Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	24.23 μM Compound: Mibefradil	Cytotoxicity against human A2780 cells after 48 hrs by MTT assay Cytotoxicity against human A2780 cells after 48 hrs by MTT assay	[PMID: 24220170]
A2780/Taxol	IC₅₀	35.26 μM Compound: Mibefradil	Cytotoxicity against human paclitaxel-resistant A2780T cells after 48 hrs by MTT assay Cytotoxicity against human paclitaxel-resistant A2780T cells after 48 hrs by MTT assay	[PMID: 24220170]
A549	IC₅₀	24.8 μM Compound: Mibefradil	Cytotoxicity against human A549 cells after 48 hrs by MTT assay Cytotoxicity against human A549 cells after 48 hrs by MTT assay	[PMID: 24529871]
A549	IC₅₀	31.4 μM Compound: Mibefradil	Cytotoxicity against human A549 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability by MTT assay	[PMID: 26739776]
A549	IC₅₀	24.9 μM Compound: Mibefradil	Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 32327350]
Caco-2	IC₅₀	1.6 μM Compound: Mibefradil	TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells	[PMID: 10901697]
Caco-2	IC₅₀	1.2 μM Compound: Mibefradil	TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells	[PMID: 11961113]
CHO	IC₅₀	3.3 μM Compound: Mibefradil	Inhibition of human ERG expressed in CHO cells by IONWORKS assay Inhibition of human ERG expressed in CHO cells by IONWORKS assay	[PMID: 23200256]
CHO	IC₅₀	0.51 μM Compound: mibefradil	Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits	[PMID: 23812503]
COS-7	IC₅₀	1430 nM Compound: 18 (Mibefradil)	K+ channel blocking activity in COS-7 African green monkey kidney derived cells expressing HERG Kv11.1 K+ channel blocking activity in COS-7 African green monkey kidney derived cells expressing HERG Kv11.1	[PMID: 12190308]
HEK293	IC₅₀	0.84 μM Compound: Midefradil	Concentration of the compounds required for inhibition of HEK293 cells (alpha1G T-type) Concentration of the compounds required for inhibition of HEK293 cells (alpha1G T-type)	[PMID: 15177437]
HEK293	IC₅₀	1.34 μM Compound: Mibefradil	Inhibition of T-type [Ca2+] channel (alpha1G) expressed in HEK293 cells Inhibition of T-type [Ca2+] channel (alpha1G) expressed in HEK293 cells	[PMID: 15603940]
HEK293	IC₅₀	1.34 μM Compound: Mibefradil	Ability to block calcium channel T type 3.1v expressed in HEK293 cells by whole cell patch clamp method Ability to block calcium channel T type 3.1v expressed in HEK293 cells by whole cell patch clamp method	[PMID: 16876404]
HEK293	IC₅₀	1.34 μM Compound: mibefradil	Inhibition of T-type calcium channel Cav3.1 expressed in HEK293 cells co-expressing alpha1G subunit by whole-cell patch clamp method Inhibition of T-type calcium channel Cav3.1 expressed in HEK293 cells co-expressing alpha1G subunit by whole-cell patch clamp method	[PMID: 17064894]
HEK293	IC₅₀	0.84 μM Compound: mibefradil	Inhibition of alpha-1G T-type calcium channel expressed in HEK293 cells by electrophysiological method Inhibition of alpha-1G T-type calcium channel expressed in HEK293 cells by electrophysiological method	[PMID: 17074493]
HEK293	IC₅₀	1.34 μM Compound: mibefradil	Inhibition of T-type calcium channel Cav3.1 expressed in HEK293 cells co-expressing alpha1G subunit and Kir2.1 potassium channel by patch-clamp assay Inhibition of T-type calcium channel Cav3.1 expressed in HEK293 cells co-expressing alpha1G subunit and Kir2.1 potassium channel by patch-clamp assay	[PMID: 17092715]
HEK293	IC₅₀	1.34 μM Compound: Mibefradil	Inhibition of T type calcium channel subunit alpha-1G expressed in HEK293 cells assessed as effect on T-type calcium currents by patch clamp method Inhibition of T type calcium channel subunit alpha-1G expressed in HEK293 cells assessed as effect on T-type calcium currents by patch clamp method	[PMID: 17150365]
HEK293	IC₅₀	1.34 μM Compound: mibefradil	Inhibition of T-type calcium channel Cav3.1 alpha-1G subunit expressed in HEK293 cells assessed as calcium current by patch-clamp assay Inhibition of T-type calcium channel Cav3.1 alpha-1G subunit expressed in HEK293 cells assessed as calcium current by patch-clamp assay	[PMID: 17869104]
HEK293	IC₅₀	0.13 μM Compound: 1, Mibefradil	Antagonist activity at human alpha1H T-type calcium channel expressed in HEK293 cells by patch clamp technique Antagonist activity at human alpha1H T-type calcium channel expressed in HEK293 cells by patch clamp technique	[PMID: 18160281]
HEK293	IC₅₀	1.34 μM Compound: mibefradil	Antagonist activity at T type calcium channel alpha1G expressed in HEK293 cells assessed as inhibition of peak currents by whole-cell patch-clamp method Antagonist activity at T type calcium channel alpha1G expressed in HEK293 cells assessed as inhibition of peak currents by whole-cell patch-clamp method	[PMID: 18625556]
HEK293	IC₅₀	1.34 μM Compound: Mibefradil	Inhibition of T-type calcium channel alpha1G expressed in human HEK293 cells assessed as inhibition of peak currents by whole-cell patch-clamp method Inhibition of T-type calcium channel alpha1G expressed in human HEK293 cells assessed as inhibition of peak currents by whole-cell patch-clamp method	[PMID: 20382529]
HEK293	IC₅₀	0.83 μM Compound: Mibefradil	Inhibition of T-type CaV3.1 channel expressed in HEK293 cells assessed as inhibition of calcium current by automated patch-clamp assay Inhibition of T-type CaV3.1 channel expressed in HEK293 cells assessed as inhibition of calcium current by automated patch-clamp assay	[PMID: 20621730]
HEK293	IC₅₀	0.86 μM Compound: Mibefradil	Inhibition of T-type CaV3.1 channel expressed in HEK293 cells assessed as inhibition of calcium current by manual patch-clamp assay Inhibition of T-type CaV3.1 channel expressed in HEK293 cells assessed as inhibition of calcium current by manual patch-clamp assay	[PMID: 20621730]
HEK293	IC₅₀	1.34 μM Compound: Mibefradil	Inhibition of T-type alpha1G channel expressed in HEK293 cells by whole-cell patch-clamp method Inhibition of T-type alpha1G channel expressed in HEK293 cells by whole-cell patch-clamp method	[PMID: 20659804]
HEK293	IC₅₀	1.34 μM Compound: Mibefradil	Inhibition of T-type alpha1G calcium channel expressed in HEK293 cells assessed as Kcl-induced depolarization Inhibition of T-type alpha1G calcium channel expressed in HEK293 cells assessed as Kcl-induced depolarization	[PMID: 21126876]
HEK293	IC₅₀	0.2 μM Compound: 1	Inhibition of human Cav3.1 alpha1G expressed in HEK293 cells assessed as inhibition of calcium influx by FLIPR assay Inhibition of human Cav3.1 alpha1G expressed in HEK293 cells assessed as inhibition of calcium influx by FLIPR assay	[PMID: 21875808]
HEK293	IC₅₀	1 μM Compound: Mibefradil	Inhibition of human T-type calcium channel Cav3.2 expressed in T-Rex293 cells by whole cell patch clamp assay Inhibition of human T-type calcium channel Cav3.2 expressed in T-Rex293 cells by whole cell patch clamp assay	[PMID: 23200256]
HEK293	IC₅₀	0.83 μM Compound: Mibefradil	Inhibition of alpha-1G calcium channel in human HEK293 cells by whole-cell patch-clamp method Inhibition of alpha-1G calcium channel in human HEK293 cells by whole-cell patch-clamp method	[PMID: 23395659]
HEK293	IC₅₀	0.56 μM Compound: Mibefradil	Inhibition of t-type Cav3.1 channel (unknown origin) expressed in HEK293 cells assessed as inhibition of 50 ms depolarizing voltage step-induced current by whole cell patch-clamp method Inhibition of t-type Cav3.1 channel (unknown origin) expressed in HEK293 cells assessed as inhibition of 50 ms depolarizing voltage step-induced current by whole cell patch-clamp method	[PMID: 24220170]
HEK293	IC₅₀	0.56 μM Compound: Mibefradil	Inhibition of T-type CaV3.1 channel (unknown origin) expressed in HEK293 cells assessed as inhibition of calcium current by whole cell patch-clamp method Inhibition of T-type CaV3.1 channel (unknown origin) expressed in HEK293 cells assessed as inhibition of calcium current by whole cell patch-clamp method	[PMID: 24529871]
HEK293	IC₅₀	1.3 μM Compound: I, Posicor	Inhibition of human ERG expressed in HEK cells by patch clamp assay Inhibition of human ERG expressed in HEK cells by patch clamp assay	[PMID: 26231163]
HEK293	IC₅₀	181 nM Compound: I, Posicor	Inhibition of recombinant Cav3.2 channel (unknown origin) expressed in HEK293 cells assessed as effect on calcium flux incubated for 3 mins by FLIPR assay Inhibition of recombinant Cav3.2 channel (unknown origin) expressed in HEK293 cells assessed as effect on calcium flux incubated for 3 mins by FLIPR assay	[PMID: 26231163]
HEK293	IC₅₀	202 nM Compound: I, Posicor	Inhibition of recombinant Cav1.2 channel (unknown origin) expressed in HEK293 cells assessed as effect on calcium flux incubated for 3 mins by FLIPR assay Inhibition of recombinant Cav1.2 channel (unknown origin) expressed in HEK293 cells assessed as effect on calcium flux incubated for 3 mins by FLIPR assay	[PMID: 26231163]
HeLa	IC₅₀	4.32 μM Compound: Mibefradil	Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay	[PMID: 29624387]
Hepatocyte	IC₅₀	0.873 nM Compound: Mibefradil	Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs	[PMID: 18212104]
LLC-PK1	IC₅₀	1.8 μM Compound: Mibefradil	Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	1.8 μM Compound: Mibefradil	TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells	[PMID: 12699389]
LLC-PK1	IC₅₀	10 μM Compound: Mibefradil	Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	10 μM Compound: Mibefradil	TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells	[PMID: 12699389]
LLC-PK1	IC₅₀	7.4 μM Compound: Mibefradil	Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	7.4 μM Compound: Mibefradil	TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells	[PMID: 12699389]
MDA-MB-231	IC₅₀	>100 μM Compound: 8	Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction in BAPTA-induced Ca2+ depletion-stimulated SOCE activity preincubated for 15 mins followed by BAPTA addition in presence of extracellular Ca2+ by PBX-ba Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction in BAPTA-induced Ca2+ depletion-stimulated SOCE activity preincubated for 15 mins followed by BAPTA addition in presence of extracellular Ca2+ by PBX-ba	[PMID: 27856238]
MDA-MB-231	IC₅₀	52.1 μM Compound: 8	Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction of SERCA inhibition-induced ER release preincubated for 15 mins followed by CPA addition by PBX-based FLIPR assay Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction of SERCA inhibition-induced ER release preincubated for 15 mins followed by CPA addition by PBX-based FLIPR assay	[PMID: 27856238]
MIA PaCa-2	IC₅₀	18.4 μM Compound: Mibefradil	Cytotoxicity against human MIAPaCa2 cells after 48 hrs by MTT assay Cytotoxicity against human MIAPaCa2 cells after 48 hrs by MTT assay	[PMID: 24529871]
SK-OV-3	IC₅₀	20.54 μM Compound: Mibefradil	Cytotoxicity against human SKOV3 cells after 48 hrs by MTT assay Cytotoxicity against human SKOV3 cells after 48 hrs by MTT assay	[PMID: 24220170]

In Vitro

Mibefradil 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.

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 (P<0.05)^[3]. Compared with the saline-treated group, rats receiving Mibefradil or Ethosuximide show significant lower Ca_V3.2 expression in the spinal cord and DRG^[4].

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

Related Protocols :

Ca²⁺ Staining Technique

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991			2011-05	PHASE1

Chemical Information

CAS No. 116644-53-2
Appearance Solid
Molecular Weight 495.63
Formula C₂₉H₃₈FN₃O₃
Color White to off-white
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
Synonyms

Ro 40-5967
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Publications (15)

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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

Electrical Stimulation Promotes Endocytosis of Magnetic Nanoparticles by Cancer Cells. [Abstract]

2024 Nov;20(46):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
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
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
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
Front Psychiatry

2026 Jun 11;17:1828920.
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
Biocell

2026 Jan 23.
Res Sq

2024 Jun 11.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

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Mibefradil

Publications Citing Use of MedChemExpress (MCE) Mibefradil

All Calcium Channel Isoforms