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Fig. 1 · Structure
Cat. No.
A12478
CAS No.
116644-53-2
Formula
C29H38FN3O3
Mol. Weight
495.63

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Mibefradil

Cat. No. A12478 CAS 116644-53-2

Calcium channel blocker

Mibefradil 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.

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Biological Activity

Cellular Effect

Cell Line Activity Value Description Reference
A2780 IC50 24.23 μM Cytotoxicity against human A2780 cells after 48 hrs by MTT assay [PMID: 24220170]
A2780/Taxol IC50 35.26 μM Cytotoxicity against human paclitaxel-resistant A2780T cells after 48 hrs by MTT assay [PMID: 24220170]
A549 IC50 24.8 μM Cytotoxicity against human A549 cells after 48 hrs by MTT assay [PMID: 24529871]
A549 IC50 24.9 μM Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay [PMID: 32327350]
A549 IC50 31.4 μM Cytotoxicity against human A549 cells assessed as reduction in cell viability by MTT assay [PMID: 26739776]
CHO IC50 0.51 μM 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]
CHO IC50 3.3 μM Inhibition of human ERG expressed in CHO cells by IONWORKS assay [PMID: 23200256]
HEK293 IC50 0.13 μM Antagonist activity at human alpha1H T-type calcium channel expressed in HEK293 cells by patch clamp technique [PMID: 18160281]
HEK293 IC50 0.2 μM Inhibition of human Cav3.1 alpha1G expressed in HEK293 cells assessed as inhibition of calcium influx by FLIPR assay [PMID: 21875808]
HEK293 IC50 0.56 μM 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 0.56 μM 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 0.83 μM Inhibition of alpha-1G calcium channel in human HEK293 cells by whole-cell patch-clamp method [PMID: 23395659]
HEK293 IC50 0.83 μM 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 0.84 μM Inhibition of alpha-1G T-type calcium channel expressed in HEK293 cells by electrophysiological method [PMID: 17074493]
HEK293 IC50 0.86 μM 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 μM Inhibition of human T-type calcium channel Cav3.2 expressed in T-Rex293 cells by whole cell patch clamp assay [PMID: 23200256]
HEK293 IC50 1.3 μM Inhibition of human ERG expressed in HEK cells by patch clamp assay [PMID: 26231163]
HEK293 IC50 1.34 μM Inhibition of T-type alpha1G channel expressed in HEK293 cells by whole-cell patch-clamp method [PMID: 20659804]
HEK293 IC50 1.34 μM 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 1.34 μM 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]

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Specifications

Manufacturer Adooq Bioscience
Actions Blocker
CAS Number 116644-53-2
Applications Calcium channel blocker
Formula C29H38FN3O3
Molecular Weight 495.63
Synonyms Ro 40-5967
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

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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