1. Membrane Transporter/Ion Channel Neuronal Signaling Metabolic Enzyme/Protease
  2. Calcium Channel P-glycoprotein Cytochrome P450
  3. Verapamil

Verapamil  (Synonyms: (±)-Verapamil; CP-16533-1)

Cat. No.: HY-14275 Purity: 99.18%
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Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research.

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

Verapamil Chemical Structure

Verapamil Chemical Structure

CAS No. : 52-53-9

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Customer Review

Based on 58 publication(s) in Google Scholar

Other Forms of Verapamil:

Top Publications Citing Use of Products

57 Publications Citing Use of MCE Verapamil

RT-PCR

    Verapamil purchased from MedChemExpress. Usage Cited in: Neurochem Res. 2022 Dec 8.  [Abstract]

    LPS-stimulated proinflammatory cytokine (IL-1β, IL-6, and TNF-α) expression and extracellular secretion in primary astrocytes are suppressed following administration of the P-gp inhibitor verapamil (Ver; 70 μM).
    • Biological Activity

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    • Customer Review

    Description

    Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research[1][2][3].

    IC50 & Target

    CYP3

     

    Cellular Effect
    Cell Line Type Value Description References
    A2780 ADR IC50
    5.2 μM
    Compound: Verapamil
    Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay
    Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay
    [PMID: 19250834]
    A2780 ADR IC50
    5.4 μM
    Compound: Verapamil
    Inhibition of P-gp expressed in A2780adr cells by calcein AM accumulation assay
    Inhibition of P-gp expressed in A2780adr cells by calcein AM accumulation assay
    [PMID: 21354800]
    A2780/Taxol IC50
    0.0188 μM
    Compound: VRP
    Reversal of multidrug resistance activity in P-gp overexpressing human A2780T cells assessed as potentiation of PTX-induced cytotoxicity by measuring PTX IC50 at 10 uM incubated for 48 hrs in presence of paclitaxel by MTT assay (Rvb = 3.972 uM)
    Reversal of multidrug resistance activity in P-gp overexpressing human A2780T cells assessed as potentiation of PTX-induced cytotoxicity by measuring PTX IC50 at 10 uM incubated for 48 hrs in presence of paclitaxel by MTT assay (Rvb = 3.972 uM)
    [PMID: 32750634]
    A2780/Taxol IC50
    18.8 nM
    Compound: Verapamil
    Potentiation of paclitaxel-induced cytotoxicity against human A2780/TAX cells assessed as paclitaxel IC50 at 10 uM after 48 hrs by MTT assay (Rvb = 3970 nM)
    Potentiation of paclitaxel-induced cytotoxicity against human A2780/TAX cells assessed as paclitaxel IC50 at 10 uM after 48 hrs by MTT assay (Rvb = 3970 nM)
    [PMID: 30455148]
    A549 IC50
    127.09 μM
    Compound: verapamil
    Cytotoxicity against taxol-resistant human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    Cytotoxicity against taxol-resistant human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    [PMID: 25582602]
    A7R5 IC50
    0.3 μM
    Compound: Verapamil
    Antagonist activity at calcium channel in rat A7R5 cells assessed as inhibition of Cacl2/KCl-induced increase in intracellular Ca2+ incubated for 15 mins prior to Cacl2/KCl challenge by fluorescence assay
    Antagonist activity at calcium channel in rat A7R5 cells assessed as inhibition of Cacl2/KCl-induced increase in intracellular Ca2+ incubated for 15 mins prior to Cacl2/KCl challenge by fluorescence assay
    [PMID: 25311564]
    B16-F10 ED50
    3 μM
    Compound: verapamil
    Inhibition of human MDR1 expressed in mouse B16/F10 cells assessed as increase in doxorubicin accumulation by fluorimetry
    Inhibition of human MDR1 expressed in mouse B16/F10 cells assessed as increase in doxorubicin accumulation by fluorimetry
    [PMID: 9461658]
    BHK-21 IC50
    ≥ 100 μM
    Compound: Verapamil
    Cytotoxicity against hamster BHK21 cells after 96 hrs by MTT assay
    Cytotoxicity against hamster BHK21 cells after 96 hrs by MTT assay
    [PMID: 20691599]
    BHK-21 IC50
    10.6 μM
    Compound: Verapamil
    Cytotoxicity against hamster BHK21 cells expressing MRP1 after 96 hrs by MTT assay
    Cytotoxicity against hamster BHK21 cells expressing MRP1 after 96 hrs by MTT assay
    [PMID: 20691599]
    Breast cancer cell line EC50
    1.2 μM
    Compound: Verapamil
    Concentration that reduces difference in reversal of [3H]VBL accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%
    Concentration that reduces difference in reversal of [3H]VBL accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%
    [PMID: 11784143]
    Breast cancer cell line EC50
    2.4 μM
    Compound: Verapamil
    Concentration that reduces the difference in reversal of DOX accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%.
    Concentration that reduces the difference in reversal of DOX accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%.
    [PMID: 11784143]
    CCRF-CEM ED50
    0.35 μM
    Compound: Verapamil
    Effective dose against CCRF-CEM vcr 100 cells by using MTT assay
    Effective dose against CCRF-CEM vcr 100 cells by using MTT assay
    [PMID: 8941391]
    CCRF-CEM ED50
    0.54 μM
    Compound: Verapamil
    Effective dose against CCRF-CEM vcr 100 cells by using rhodamine efflux studies.
    Effective dose against CCRF-CEM vcr 100 cells by using rhodamine efflux studies.
    [PMID: 8941391]
    CHO IC50
    0.2 μM
    Compound: verapamil
    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]
    CHO IC50
    0.53 μM
    Compound: Verapamil
    Inhibition of human ERG expressed in CHO cells at holding potential of -90 mV by patch clamp method
    Inhibition of human ERG expressed in CHO cells at holding potential of -90 mV by patch clamp method
    [PMID: 28797771]
    CHO IC50
    0.56 μM
    Compound: Verapamil
    Cytotoxicity against CHO cells by MTT assay
    Cytotoxicity against CHO cells by MTT assay
    [PMID: 30429978]
    CHO IC50
    23.5 μM
    Compound: Verapamil
    Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Chinese hamster ovary cells heterologically expressing alpha-1C subunit
    Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Chinese hamster ovary cells heterologically expressing alpha-1C subunit
    [PMID: 22761000]
    ECa-109 cell line IC50
    679 nM
    Compound: VRP
    Reversal of VCR -resistance in human Eca-109 cells assessed as vincristine IC50 by measuring cell viability incubated for 48 hrs by CCK-8 method (Rvb = 6830.0+/-537.0 nM)
    Reversal of VCR -resistance in human Eca-109 cells assessed as vincristine IC50 by measuring cell viability incubated for 48 hrs by CCK-8 method (Rvb = 6830.0+/-537.0 nM)
    [PMID: 36892076]
    ECa-109 cell line IC50
    679 nM
    Compound: VRP
    Reversal of VCR -resistance in human Eca-109 cells assessed as cell viability at 5 uM incubated for 48 hrs by CCK-8 method (Rvb = 6830.0+/-537.0 nM)
    Reversal of VCR -resistance in human Eca-109 cells assessed as cell viability at 5 uM incubated for 48 hrs by CCK-8 method (Rvb = 6830.0+/-537.0 nM)
    [PMID: 36892076]
    Flp-In-293 IC50
    > 50 μM
    Compound: Verapamil
    Cytotoxicity against Flp-In-293 cells assessed as reduction in cell viability measured after 72 hrs by SRB assay
    Cytotoxicity against Flp-In-293 cells assessed as reduction in cell viability measured after 72 hrs by SRB assay
    [PMID: 32569926]
    Flp-In-293 IC50
    > 50 μM
    Compound: Verapamil
    Cytotoxicity against Flp-In-293 cells expressing human ABCB1 assessed as reduction in cell viability measured after 72 hrs by SRB assay
    Cytotoxicity against Flp-In-293 cells expressing human ABCB1 assessed as reduction in cell viability measured after 72 hrs by SRB assay
    [PMID: 32569926]
    HEK293 IC50
    > 50 μM
    Compound: Verapamil
    Cytotoxicity against human Flp-In-293 cells assessed as reduction in cell viability by SRB assay
    Cytotoxicity against human Flp-In-293 cells assessed as reduction in cell viability by SRB assay
    [PMID: 27810590]
    HEK293 IC50
    > 50 μM
    Compound: Verapamil
    Cytotoxicity against human Flp-In-293 cells expressing MDR1 assessed as reduction in cell viability by SRB assay
    Cytotoxicity against human Flp-In-293 cells expressing MDR1 assessed as reduction in cell viability by SRB assay
    [PMID: 27810590]
    HEK293 IC50
    > 600 μM
    Compound: Verapamil
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate
    [PMID: 22587986]
    HEK293 IC50
    1.62 nM
    Compound: VPM
    Reversal of resistance to paclitaxel-induced cytotoxicity in HEK293 cells assessed as paclitaxel IC50 at 4 uM pre-incubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb =1.93 +/- 0.06 nM)
    Reversal of resistance to paclitaxel-induced cytotoxicity in HEK293 cells assessed as paclitaxel IC50 at 4 uM pre-incubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb =1.93 +/- 0.06 nM)
    [PMID: 33280384]
    HEK293 IC50
    1.62 μM
    Compound: Verapamil
    Reversal of resistance to paclitaxel-induced cytotoxicity in human HEK293/pcDNA3.1 cells assessed as reduction in paclitaxel IC50 at 4 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 1.93 +/- 0.06 nM
    Reversal of resistance to paclitaxel-induced cytotoxicity in human HEK293/pcDNA3.1 cells assessed as reduction in paclitaxel IC50 at 4 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 1.93 +/- 0.06 nM
    [PMID: 34723530]
    HEK293 IC50
    10.37 μM
    Compound: Verapamil
    Reversal of resistance to paclitaxel-induced cytotoxicity in human HEK293/ABCB1 cells assessed as reduction in paclitaxel IC50 at 4 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 91.40 +/- 23.32 nM)
    Reversal of resistance to paclitaxel-induced cytotoxicity in human HEK293/ABCB1 cells assessed as reduction in paclitaxel IC50 at 4 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 91.40 +/- 23.32 nM)
    [PMID: 34723530]
    HEK293 IC50
    101.26 μM
    Compound: VRP
    Cytotoxicity against HEK293 cells after 48 hrs by MTT assay
    Cytotoxicity against HEK293 cells after 48 hrs by MTT assay
    [PMID: 29407947]
    HEK293 IC50
    24 μM
    Compound: Verapamil
    Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
    Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
    [PMID: 22761000]
    HEK293 CC50
    280 μM
    Compound: Verapamil
    Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    [PMID: 30108738]
    HEK293 IC50
    32 μM
    Compound: Verapamil
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate
    [PMID: 22587986]
    HEK293 IC50
    41500 nM
    Compound: Verapamil
    Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA
    Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA
    [PMID: 21300721]
    HEK293 IC50
    47 μM
    Compound: Verapamil
    Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
    Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
    [PMID: 22761000]
    HEK293 IC50
    50 μM
    Compound: Verapamil
    Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
    Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
    [PMID: 22761000]
    HEK293 IC50
    6.8 μM
    Compound: verapamil
    Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
    Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
    [PMID: 18788725]
    HEK293 IC50
    64 μM
    Compound: Verapamil
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate
    [PMID: 22587986]
    HEK-293T IC50
    32.04 μM
    Compound: Verapamil
    Cytotoxicity against human HEK293T cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Cytotoxicity against human HEK293T cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    [PMID: 36242992]
    HeLa IC50
    > 50 μM
    Compound: Verapamil
    Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by SRB assay
    Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by SRB assay
    [PMID: 32569926]
    HeLa IC50
    1.7 μM
    Compound: verapamil
    Inhibition of P-glycoprotein 1 in human HeLa cells assessed as intracellular accumulation of Hoechst 33342 dye after 30 mins by fluorescence microscopic analysis
    Inhibition of P-glycoprotein 1 in human HeLa cells assessed as intracellular accumulation of Hoechst 33342 dye after 30 mins by fluorescence microscopic analysis
    10.1039/C2MD20286G
    HeLa S3 IC50
    > 50 μM
    Compound: Verapamil
    Cytotoxicity against human HeLaS3 assessed as reduction in cell viability by SRB assay
    Cytotoxicity against human HeLaS3 assessed as reduction in cell viability by SRB assay
    [PMID: 27810590]
    HepG2 IC50
    138.42 μM
    Compound: VRP
    Cytotoxicity against adriamycin-resistant human HepG2 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay
    Cytotoxicity against adriamycin-resistant human HepG2 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay
    [PMID: 27328029]
    HepG2 IC50
    65.2 μM
    Compound: Verapamil
    Cytotoxicity in human HepG2 cells assessed as number of live cells by measuring ATP metabolism incubated for 48 hrs by CellTiter-Glo luminescent cell viability assay
    Cytotoxicity in human HepG2 cells assessed as number of live cells by measuring ATP metabolism incubated for 48 hrs by CellTiter-Glo luminescent cell viability assay
    [PMID: 36367749]
    HL-60 EC50
    1.8 μg/mL
    Compound: Verapamil
    Effective concentration against HL-60/ADR cells using MRP-mediated MDR assay using 2 nM vincristine which results in 50% of the cells being killed in the presence of particular cytotoxic drug.
    Effective concentration against HL-60/ADR cells using MRP-mediated MDR assay using 2 nM vincristine which results in 50% of the cells being killed in the presence of particular cytotoxic drug.
    [PMID: 9526572]
    K562 IC50
    > 100 μM
    Compound: VRP
    Cytotoxicity against human K562 cells incubated for 48 hrs by MTT assay
    Cytotoxicity against human K562 cells incubated for 48 hrs by MTT assay
    [PMID: 33938746]
    K562 IC50
    0.029 μM
    Compound: Verapamil
    Modulatory activity at P-gp assessed as doxorubicin IC50 in human K562 cells at 3 uM after 72 hrs by MTT assay (Rvb doxorubicin alone IC50 = 0.023 +/- 0.004 uM)
    Modulatory activity at P-gp assessed as doxorubicin IC50 in human K562 cells at 3 uM after 72 hrs by MTT assay (Rvb doxorubicin alone IC50 = 0.023 +/- 0.004 uM)
    [PMID: 25282263]
    K562 IC50
    1.6 μM
    Compound: Verapamil
    Inhibition of Pgp-mediated multidrug resistance in doxorubicin-resistant human K562 cells assessed as drug level required for 50% increase in nuclear concentration of pirarubicin by fluorescence assay
    Inhibition of Pgp-mediated multidrug resistance in doxorubicin-resistant human K562 cells assessed as drug level required for 50% increase in nuclear concentration of pirarubicin by fluorescence assay
    [PMID: 21145739]
    K562 IC50
    1.6 μM
    Compound: Verapamil
    Inhibition of P-glycoprotein in human doxorubicin-resistant K562 cells assessed as half maximal increase of pirarubicin accumulation by spectrofluorometric analysis
    Inhibition of P-glycoprotein in human doxorubicin-resistant K562 cells assessed as half maximal increase of pirarubicin accumulation by spectrofluorometric analysis
    [PMID: 23245571]
    K562 IC50
    36.7 μM
    Compound: VRP
    Cytotoxicity against human K562 cells after 48 hrs by MTT assay
    Cytotoxicity against human K562 cells after 48 hrs by MTT assay
    [PMID: 28301155]
    K562 IC50
    37 μM
    Compound: verapamil
    Ability to potentiate DOX cytotoxicity on K562/DOX MDR cells. Cell survival was assayed by MTT conversion
    Ability to potentiate DOX cytotoxicity on K562/DOX MDR cells. Cell survival was assayed by MTT conversion
    [PMID: 9986718]
    K562 IC50
    65.28 μM
    Compound: VRP
    Cytotoxicity against human K562 cells after 48 hrs by MTT assay
    Cytotoxicity against human K562 cells after 48 hrs by MTT assay
    [PMID: 28645831]
    K562 IC50
    65.28 μM
    Compound: VRP
    Cytotoxicity against human K562 cells assessed as cell viability after 48 hrs by MTT assay
    Cytotoxicity against human K562 cells assessed as cell viability after 48 hrs by MTT assay
    [PMID: 27073052]
    K562 IC50
    68.27 μM
    Compound: VRP
    Cytotoxicity against human K562 cells assessed as cell growth inhibition after 48 hrs by MTT assay
    Cytotoxicity against human K562 cells assessed as cell growth inhibition after 48 hrs by MTT assay
    [PMID: 31202598]
    K562 IC50
    68.92 μM
    Compound: VRP
    Cytotoxicity against human K562 cells after 48 hrs by MTT assay
    Cytotoxicity against human K562 cells after 48 hrs by MTT assay
    [PMID: 35247755]
    K562 IC50
    82.2 μM
    Compound: VRP
    Cytotoxicity against human K562 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    Cytotoxicity against human K562 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    [PMID: 29631786]
    K562/A02 IC50
    > 100 μM
    Compound: VRP
    Cytotoxicity against P-gp overexpressing human K562/A02 cells incubated for 48 hrs by MTT assay
    Cytotoxicity against P-gp overexpressing human K562/A02 cells incubated for 48 hrs by MTT assay
    [PMID: 33938746]
    K562/A02 IC50
    31.28 μM
    Compound: VRP
    Cytotoxicity against human K562/A02 cells overexpressing P-gp after 48 hrs by MTT assay
    Cytotoxicity against human K562/A02 cells overexpressing P-gp after 48 hrs by MTT assay
    [PMID: 28301155]
    K562/A02 IC50
    39.86 μM
    Compound: VRP
    Cytotoxicity against human K562/A02 cells after 48 hrs by MTT assay
    Cytotoxicity against human K562/A02 cells after 48 hrs by MTT assay
    [PMID: 35247755]
    K562/A02 IC50
    56.24 μM
    Compound: VRP
    Cytotoxicity against human K562/A02 cells after 48 hrs by MTT assay
    Cytotoxicity against human K562/A02 cells after 48 hrs by MTT assay
    [PMID: 28645831]
    K562/A02 IC50
    56.24 μM
    Compound: VRP
    Cytotoxicity against human K562/A02 cells assessed as cell viability after 48 hrs by MTT assay
    Cytotoxicity against human K562/A02 cells assessed as cell viability after 48 hrs by MTT assay
    [PMID: 27073052]
    K562/A02 IC50
    59.24 μM
    Compound: VRP
    Cytotoxicity against human K562/A02 cells overexpressing P-gp assessed as cell growth inhibition after 48 hrs by MTT assay
    Cytotoxicity against human K562/A02 cells overexpressing P-gp assessed as cell growth inhibition after 48 hrs by MTT assay
    [PMID: 31202598]
    K562/A02 IC50
    67.2 μM
    Compound: VRP
    Cytotoxicity against human K562/A02 cells overexpressing P-gp assessed as reduction in cell viability after 48 hrs by MTT assay
    Cytotoxicity against human K562/A02 cells overexpressing P-gp assessed as reduction in cell viability after 48 hrs by MTT assay
    [PMID: 29631786]
    K562/Adr IC50
    0.74 μM
    Compound: Verapamil
    Modulatory activity at P-gp assessed as doxorubicin IC50 in human K562/DOX cells at 3 uM after 72 hrs by MTT assay (Rvb doxorubicin alone IC50 = 2.00 +/- 0.24 uM)
    Modulatory activity at P-gp assessed as doxorubicin IC50 in human K562/DOX cells at 3 uM after 72 hrs by MTT assay (Rvb doxorubicin alone IC50 = 2.00 +/- 0.24 uM)
    [PMID: 25282263]
    K562/Adr IC50
    1.6 μM
    Compound: Verapamil
    Modulatory activity at P-gp in human K562/DOX cells assessed as increase in nuclear concentration of pirarubicin by spectrofluorometric assay
    Modulatory activity at P-gp in human K562/DOX cells assessed as increase in nuclear concentration of pirarubicin by spectrofluorometric assay
    [PMID: 25282263]
    K562/R7 IC50
    0.6 μM
    Compound: verapamil
    Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay
    Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay
    [PMID: 25634041]
    KB IC50
    > 25 μg/mL
    Compound: Verapamil
    Cytotoxicity against human vincristine-sensitive KB cells assessed as cell viability after 72 hrs by MTT assay
    Cytotoxicity against human vincristine-sensitive KB cells assessed as cell viability after 72 hrs by MTT assay
    [PMID: 26717050]
    KB IC50
    19.6 μM
    Compound: VRM (verapamil)
    Inhibitory activity against KB cell line after 72 h of drug exposure
    Inhibitory activity against KB cell line after 72 h of drug exposure
    [PMID: 15481991]
    KB 3-1 IC50
    0.0047 μM
    Compound: verapamil
    Reversal of P-gp-mediated multidrug resistance to Cytotoxicity of colchicine against human KB-3-1 cells at 5 uM after 68 hrs by MTT assay
    Reversal of P-gp-mediated multidrug resistance to Cytotoxicity of colchicine against human KB-3-1 cells at 5 uM after 68 hrs by MTT assay
    [PMID: 17488128]
    KB 3-1 IC50
    20.5 μg/mL
    Compound: verapamil
    Cytotoxicity against human KB31 cells after 48 hrs by SRB assay
    Cytotoxicity against human KB31 cells after 48 hrs by SRB assay
    [PMID: 10217732]
    KB 3-1 IC50
    3.84 nM
    Compound: VPM
    Reversal of resistance to paclitaxel-induced cytotoxicity in human KB 3-1 cells assessed as paclitaxel IC50 at 4 uM pre-incubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 4.54 +/- 1.59 nM)
    Reversal of resistance to paclitaxel-induced cytotoxicity in human KB 3-1 cells assessed as paclitaxel IC50 at 4 uM pre-incubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 4.54 +/- 1.59 nM)
    [PMID: 33280384]
    KB 3-1 IC50
    3.84 μM
    Compound: Verapamil
    Reversal of resistance to paclitaxel-induced cytotoxicity in human KB 3-1 cells assessed as reduction in paclitaxel IC50 at 4 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 4.54 +/- 1.59 nM)
    Reversal of resistance to paclitaxel-induced cytotoxicity in human KB 3-1 cells assessed as reduction in paclitaxel IC50 at 4 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 4.54 +/- 1.59 nM)
    [PMID: 34723530]
    KB 3-1 IC50
    45.2 μM
    Compound: VRP
    Cytotoxicity against human KB31 cells after 48 hrs by SRB method
    Cytotoxicity against human KB31 cells after 48 hrs by SRB method
    [PMID: 10346948]
    KB 3-1 IC50
    51.7 μM
    Compound: VRM (verapamil)
    Inhibitory activity against KB/MDR cell line after 72 hr of drug exposure
    Inhibitory activity against KB/MDR cell line after 72 hr of drug exposure
    [PMID: 15481991]
    KB/VJ300 IC50
    > 10 μM
    Compound: Verapamil
    Growth inhibition of human KB/VJ300 cells after 72 hrs by MTT assay
    Growth inhibition of human KB/VJ300 cells after 72 hrs by MTT assay
    [PMID: 26918761]
    KB/VJ300 IC50
    > 25 μg/mL
    Compound: Verapamil
    Cytotoxicity against human KB/VJ300 cells assessed as cell viability after 72 hrs by MTT assay
    Cytotoxicity against human KB/VJ300 cells assessed as cell viability after 72 hrs by MTT assay
    [PMID: 26717050]
    KB/VJ300 IC50
    0.1 μM
    Compound: Verapamil
    Growth inhibition of human KB/VJ300 cells after 72 hrs in presence of 0.1 uM of vincristine by MTT assay
    Growth inhibition of human KB/VJ300 cells after 72 hrs in presence of 0.1 uM of vincristine by MTT assay
    [PMID: 29746134]
    KB/VJ300 IC50
    0.4 μM
    Compound: Verapamil
    Antiproliferative activity against human vincristine-rsistant KB/VJ300 cells assessed as reduction in cell growth after 72 hrs by MTT assay
    Antiproliferative activity against human vincristine-rsistant KB/VJ300 cells assessed as reduction in cell growth after 72 hrs by MTT assay
    [PMID: 31642315]
    KB/VJ300 IC50
    0.8 μM
    Compound: Verapamil
    Cytotoxicity against human KB/VJ300 cells after 72 hrs in presence of vincristine by MTT assay
    Cytotoxicity against human KB/VJ300 cells after 72 hrs in presence of vincristine by MTT assay
    [PMID: 30869890]
    KB/VJ300 IC50
    10.3 μM
    Compound: Verapamil
    Cytotoxicity against human KB/VJ300 cells assessed as cell viability after 72 hrs by MTT assay in presence of 0.121 uM vincristine
    Cytotoxicity against human KB/VJ300 cells assessed as cell viability after 72 hrs by MTT assay in presence of 0.121 uM vincristine
    [PMID: 26717050]
    KB/VJ300 IC50
    4.6 μM
    Compound: Verapamil
    Growth inhibition of human KB/VJ300 cells after 72 hrs in presence of vincristine by MTT assay
    Growth inhibition of human KB/VJ300 cells after 72 hrs in presence of vincristine by MTT assay
    [PMID: 26918761]
    KB-C2 IC50
    7.05 μM
    Compound: Verapamil
    Reversal of resistance to paclitaxel-induced cytotoxicity in human KB-C2 cells assessed as reduction in paclitaxel IC50 at 4 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 1886.37 +/- 243.05 nM)
    Reversal of resistance to paclitaxel-induced cytotoxicity in human KB-C2 cells assessed as reduction in paclitaxel IC50 at 4 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 1886.37 +/- 243.05 nM)
    [PMID: 34723530]
    KB-V1 IC50
    0.69 μg/mL
    Compound: verapamil
    Cytotoxicity against human KBV1 cells after 48 hrs by SRB assay in presence of vinblastine
    Cytotoxicity against human KBV1 cells after 48 hrs by SRB assay in presence of vinblastine
    [PMID: 10217732]
    KB-V1 IC50
    1.6 μM
    Compound: VRP
    Cytotoxicity against vinblastine resistant human KBV1 cells after 48 hrs in presence of 100 nM vinblastine by SRB method
    Cytotoxicity against vinblastine resistant human KBV1 cells after 48 hrs in presence of 100 nM vinblastine by SRB method
    [PMID: 10346948]
    KB-V1 IC50
    15.3 μg/mL
    Compound: verapamil
    Cytotoxicity against human KBV1 cells after 48 hrs by SRB assay
    Cytotoxicity against human KBV1 cells after 48 hrs by SRB assay
    [PMID: 10217732]
    KB-V1 IC50
    39.2 μM
    Compound: VRP
    Cytotoxicity against vinblastine resistant human KBV1 cells after 48 hrs by SRB method
    Cytotoxicity against vinblastine resistant human KBV1 cells after 48 hrs by SRB method
    [PMID: 10346948]
    L5178Y IC50
    > 100 nM
    Compound: VER
    Cytotoxicity against mouse L5178Y cells assessed as reduction in cell viability by MTT assay
    Cytotoxicity against mouse L5178Y cells assessed as reduction in cell viability by MTT assay
    [PMID: 32871268]
    L5178Y IC50
    > 100 μM
    Compound: VP
    Cytotoxicity against mouse L5178Y cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against mouse L5178Y cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 27156771]
    L5178Y IC50
    47.85 nM
    Compound: VER
    Cytotoxicity against multidrug resistance mouse L5178Y cells expressing human MDR1 assessed as reduction in cell viability by MTT assay
    Cytotoxicity against multidrug resistance mouse L5178Y cells expressing human MDR1 assessed as reduction in cell viability by MTT assay
    [PMID: 32871268]
    L5178Y IC50
    47.85 μM
    Compound: VP
    Cytotoxicity against multi-drug resistant mouse L5178Y cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against multi-drug resistant mouse L5178Y cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 27156771]
    L929 IC50
    8 μM
    Compound: Verapamil
    Inhibition of Kv1.3 expressed in mouse L929 cells exposed to depolarizing step pulses from -80 mV to +40 mV by whole cell patch clamp method
    Inhibition of Kv1.3 expressed in mouse L929 cells exposed to depolarizing step pulses from -80 mV to +40 mV by whole cell patch clamp method
    [PMID: 23084278]
    L929 IC50
    88 μM
    Compound: Verapamil
    Cytotoxicity against mouse L929 cells assessed as reduction in cell survival after 5 days by MTS assay
    Cytotoxicity against mouse L929 cells assessed as reduction in cell survival after 5 days by MTS assay
    [PMID: 30351934]
    L929 IC50
    89 μM
    Compound: Verapamil
    Cytotoxicity against mouse L929 cells measured after 3 days by MTS assay
    Cytotoxicity against mouse L929 cells measured after 3 days by MTS assay
    [PMID: 27750197]
    L929 IC50
    89 μM
    Compound: Verapamil
    Cytotoxicity against mouse L929 cells assessed as cell survival after 3 days by MTS/PMS assay
    Cytotoxicity against mouse L929 cells assessed as cell survival after 3 days by MTS/PMS assay
    [PMID: 26233798]
    L929 IC50
    89.2 μM
    Compound: Verapamil
    Cytotoxicity against mouse L929 cells after 3 days by MTS assay
    Cytotoxicity against mouse L929 cells after 3 days by MTS assay
    [PMID: 25985195]
    L929 IC50
    89.2 μM
    Compound: verapamil
    Cytotoxicity against mouse L929 cells assessed as growth inhibition after 3 days by MTS assay
    Cytotoxicity against mouse L929 cells assessed as growth inhibition after 3 days by MTS assay
    [PMID: 24171478]
    L929 IC50
    89.2 μM
    Compound: Verapamil
    Cytotoxicity against mouse L929 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
    Cytotoxicity against mouse L929 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
    [PMID: 34597896]
    L929 IC50
    89.2 μM
    Compound: 1
    Cytotoxicity against mouse L929 cells after 72 hrs
    Cytotoxicity against mouse L929 cells after 72 hrs
    [PMID: 22320402]
    LLC-PK1 IC50
    10 μM
    Compound: Verapamil
    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
    2 μM
    Compound: Verapamil
    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
    6.3 μM
    Compound: Verapamil
    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]
    Macrophage cell line CC50
    116.6 μM
    Compound: VP
    Cytotoxicity in human monocyte-derived macrophages assessed as reduction in cell viability incubated for 3 days by alamar blue dye based assay
    Cytotoxicity in human monocyte-derived macrophages assessed as reduction in cell viability incubated for 3 days by alamar blue dye based assay
    [PMID: 28964936]
    MCF7 EC50
    1 μg/mL
    Compound: Verapamil
    Effective concentration against MCF-7/ADR cells using P-gp-mediated MDR assay using 25 nM actinomycin D which results in 50% of the cells being killed in the presence of particular cytotoxic drug.
    Effective concentration against MCF-7/ADR cells using P-gp-mediated MDR assay using 25 nM actinomycin D which results in 50% of the cells being killed in the presence of particular cytotoxic drug.
    [PMID: 9526572]
    MCF7 IC50
    1.5 μM
    Compound: Verapamil
    Potentiation of adriamycin-induced cytotoxicity in human MCF7 cells assessed as adriamycin IC50 at 10 ug/ml after 48 hrs by MTT assay (Rvb = 1.3 +/- 0.2 uM)
    Potentiation of adriamycin-induced cytotoxicity in human MCF7 cells assessed as adriamycin IC50 at 10 ug/ml after 48 hrs by MTT assay (Rvb = 1.3 +/- 0.2 uM)
    [PMID: 30137985]
    MCF7 IC50
    48.91 μM
    Compound: VRP
    Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
    Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
    [PMID: 29407947]
    MCF7 IC50
    87.83 μM
    Compound: Verapamil
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    [PMID: 36242992]
    MDA-MB-435 IC50
    0.25 nM
    Compound: Verapamil
    Reversal of vinblastine resistance in multidrug resistant MDA435/LCC6 cells by MTS assay
    Reversal of vinblastine resistance in multidrug resistant MDA435/LCC6 cells by MTS assay
    [PMID: 17154505]
    MDA-MB-435 EC50
    0.7 μM
    Compound: Verapamil
    Reversal of paclitaxel resistance in multidrug resistant MDA435/LCC6 cells by MTS assay
    Reversal of paclitaxel resistance in multidrug resistant MDA435/LCC6 cells by MTS assay
    [PMID: 17154505]
    MDA-MB-435 IC50
    5.2 nM
    Compound: Verapamil
    Reversal of paclitaxel resistance in multidrug resistant MDA435/LCC6 cells by MTS assay
    Reversal of paclitaxel resistance in multidrug resistant MDA435/LCC6 cells by MTS assay
    [PMID: 17154505]
    MDCK IC50
    0.5 μM
    Compound: Ver
    Inhibition of human MDR1 expressed in MDCK cells assessed as calcein AM accumulation after 30 mins by fluorescence assay
    Inhibition of human MDR1 expressed in MDCK cells assessed as calcein AM accumulation after 30 mins by fluorescence assay
    [PMID: 22112208]
    MDCK EC50
    0.9 μM
    Compound: Ver
    Inhibition of BCRP (unknown origin) expressed in MDCK cells assessed as increase in Hoechst 33342 accumulation incubated for 30 mins by Hoechst 33342 dye based fluorescence assay
    Inhibition of BCRP (unknown origin) expressed in MDCK cells assessed as increase in Hoechst 33342 accumulation incubated for 30 mins by Hoechst 33342 dye based fluorescence assay
    [PMID: 31494468]
    MDCK IC50
    1.3 μM
    Compound: Verapamil
    Inhibition of MDR1 (unknown origin) expressed in MDCK cells assessed as reduction in calcein-AM efflux preincubated for 30 mins followed by calcein-AM addition measured after 30 mins by spectrofluorimetric method
    Inhibition of MDR1 (unknown origin) expressed in MDCK cells assessed as reduction in calcein-AM efflux preincubated for 30 mins followed by calcein-AM addition measured after 30 mins by spectrofluorimetric method
    [PMID: 30384046]
    MDCK EC50
    20 μM
    Compound: Verapamil
    Inhibition of P-glycoprotein (unknown origin) expressed in MDCK cells assessed as reduction of calcein-AM transport after 30 mins by fluorescence assay
    Inhibition of P-glycoprotein (unknown origin) expressed in MDCK cells assessed as reduction of calcein-AM transport after 30 mins by fluorescence assay
    [PMID: 24607999]
    MDCK IC50
    3.5 μM
    Compound: Verapamil
    Inhibition of MRP1 (unknown origin) expressed in MDCK cells after 30 mins by Calcein-AM assay
    Inhibition of MRP1 (unknown origin) expressed in MDCK cells after 30 mins by Calcein-AM assay
    [PMID: 25093931]
    MDCK IC50
    4.5 μM
    Compound: Verapamil
    Inhibition of MRP1 (unknown origin) expressed in MDCK cells assessed as reduction in calcein-AM efflux preincubated for 30 mins followed by calcein-AM addition measured after 30 mins by spectrofluorimetric method
    Inhibition of MRP1 (unknown origin) expressed in MDCK cells assessed as reduction in calcein-AM efflux preincubated for 30 mins followed by calcein-AM addition measured after 30 mins by spectrofluorimetric method
    [PMID: 30384046]
    MDCK IC50
    6.8 μM
    Compound: Ver
    Inhibition of MRP1 expressed in MDCK cells assessed as calcein AM accumulation after 30 mins by fluorescence assay
    Inhibition of MRP1 expressed in MDCK cells assessed as calcein AM accumulation after 30 mins by fluorescence assay
    [PMID: 22112208]
    MDCK EC50
    6.8 μM
    Compound: Ver
    Inhibition of MRP1 (unknown origin) expressed in MDCK cells assessed as increase in calcein-AM accumulation incubated for 30 mins by calcein-AM dye based fluorescence assay
    Inhibition of MRP1 (unknown origin) expressed in MDCK cells assessed as increase in calcein-AM accumulation incubated for 30 mins by calcein-AM dye based fluorescence assay
    [PMID: 31494468]
    MDCK IC50
    9.8 μM
    Compound: Verapamil
    Inhibition of MDR1 expressed in MDCK cells using rhodamine 123 staining by flow cytometry
    Inhibition of MDR1 expressed in MDCK cells using rhodamine 123 staining by flow cytometry
    [PMID: 21354800]
    MDCK-II IC50
    > 100 μM
    Compound: VRP
    Cytotoxicity against MDCK-II cells incubated for 48 hrs by MTT assay
    Cytotoxicity against MDCK-II cells incubated for 48 hrs by MTT assay
    [PMID: 33938746]
    MDCK-II IC50
    > 100 μM
    Compound: VRP
    Cytotoxicity against BCRP-overexpressing MDCK-II cells incubated for 48 hrs by MTT assay
    Cytotoxicity against BCRP-overexpressing MDCK-II cells incubated for 48 hrs by MTT assay
    [PMID: 33938746]
    MDCK-II IC50
    14 μM
    Compound: VER
    Inhibition of human MDR1 expressed in MDCK2 cells assessed as enhancement of Calcein-AM uptake treated 30 mins before Calcein-AM challenge measured after 20 mins
    Inhibition of human MDR1 expressed in MDCK2 cells assessed as enhancement of Calcein-AM uptake treated 30 mins before Calcein-AM challenge measured after 20 mins
    [PMID: 19402665]
    MDCK-II EC50
    5.1 μM
    Compound: VER
    Enhancement of calcein-AM uptake in MDCK2 cells over expressing MDR1 after 20 mins
    Enhancement of calcein-AM uptake in MDCK2 cells over expressing MDR1 after 20 mins
    [PMID: 18849167]
    MDCK-MDR1 EC50
    0.5 μM
    Compound: Ver
    Inhibition of P-glycoprotein (unknown origin) in MDCK-MDR1 assessed as inhibtion of calcein-AM transport incubated for 30 mins by fluorescence assay
    Inhibition of P-glycoprotein (unknown origin) in MDCK-MDR1 assessed as inhibtion of calcein-AM transport incubated for 30 mins by fluorescence assay
    [PMID: 30947123]
    MDCK-MDR1 EC50
    0.5 μM
    Compound: Ver
    Inhibition of P-gp (unknown origin) expressed in MDCK-MDR1 cells assessed as increase in calcein-AM accumulation incubated for 30 mins by calcein-AM dye based fluorescence assay
    Inhibition of P-gp (unknown origin) expressed in MDCK-MDR1 cells assessed as increase in calcein-AM accumulation incubated for 30 mins by calcein-AM dye based fluorescence assay
    [PMID: 31494468]
    MDCK-MDR1 EC50
    6.8 μM
    Compound: Ver
    Inhibition of MRP1 (unknown origin) in MDCK-MDR1 assessed as inhibtion of calcein-AM transport incubated for 30 mins by fluorescence assay
    Inhibition of MRP1 (unknown origin) in MDCK-MDR1 assessed as inhibtion of calcein-AM transport incubated for 30 mins by fluorescence assay
    [PMID: 30947123]
    MES-SA EC50
    37.3 μM
    Compound: Verapamil
    Modulation of BCRP1 mediated drug efflux in mitoxantrone-resistant human MES-SA cells assessed as accumulation of hoechst 33342 incubated for 15 mins prior to rhodamine-123 addition measured after 90 mins by fluorescence analysis
    Modulation of BCRP1 mediated drug efflux in mitoxantrone-resistant human MES-SA cells assessed as accumulation of hoechst 33342 incubated for 15 mins prior to rhodamine-123 addition measured after 90 mins by fluorescence analysis
    [PMID: 25311564]
    MES-SA EC50
    7.1 μM
    Compound: Verapamil
    Modulation of P-gp mediated drug efflux in human MES-SA cells assessed as accumulation of rhodamine-123 incubated for 15 mins prior to rhodamine-123 addition measured after 1 hr by fluorescence analysis
    Modulation of P-gp mediated drug efflux in human MES-SA cells assessed as accumulation of rhodamine-123 incubated for 15 mins prior to rhodamine-123 addition measured after 1 hr by fluorescence analysis
    [PMID: 25311564]
    NCI/ADR-RES IC50
    > 100 μM
    Compound: Verapamil
    Antiproliferative activity against human multidrug resistant NCI-ADR-RES cells overexpressing P-gp assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Antiproliferative activity against human multidrug resistant NCI-ADR-RES cells overexpressing P-gp assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    [PMID: 36242992]
    NCI/ADR-RES IC50
    > 100 μM
    Compound: Verapamil
    Cytotoxicity against human MCF7/ADR cells after 72 hrs by MTT assay
    Cytotoxicity against human MCF7/ADR cells after 72 hrs by MTT assay
    [PMID: 19523827]
    NCI/ADR-RES IC50
    > 150 μM
    Compound: VRP
    Intrinsic cytotoxicity against human MCF7/ADR cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay
    Intrinsic cytotoxicity against human MCF7/ADR cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay
    [PMID: 27328029]
    NCI/ADR-RES IC50
    2.24 μM
    Compound: Verapamil
    Reversal of P-gp-mediated multidrug resistance in human NCI-ADR-RES cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 10 uM incubated for 48 hrs by MTT assay
    Reversal of P-gp-mediated multidrug resistance in human NCI-ADR-RES cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 10 uM incubated for 48 hrs by MTT assay
    [PMID: 36242992]
    NCI/ADR-RES IC50
    2.25 μM
    Compound: VRP
    Potentiation of adriamycin-induced antiproliferative activity against human MCF7/ADR cells assessed as adriamycin IC50 at 5 uM measured after 48 hrs by MTT assay (Rvb = 89.14 +/- 4.89 uM)
    Potentiation of adriamycin-induced antiproliferative activity against human MCF7/ADR cells assessed as adriamycin IC50 at 5 uM measured after 48 hrs by MTT assay (Rvb = 89.14 +/- 4.89 uM)
    [PMID: 30837097]
    NCI/ADR-RES IC50
    2.83 μM
    Compound: VRP
    Reversal of multidrug resistant activity in human MCF7/ADR cells after 48 hrs by MTT assay
    Reversal of multidrug resistant activity in human MCF7/ADR cells after 48 hrs by MTT assay
    [PMID: 35339100]
    NCI/ADR-RES EC50
    321.83 nM
    Compound: Verapamil
    Reversal of P-gp-mediated multidrug resistance in human NCI-ADR-RES cells assessed as potentiation of doxorubicin-induced cytotoxicity incubated for 48 hrs by MTT assay
    Reversal of P-gp-mediated multidrug resistance in human NCI-ADR-RES cells assessed as potentiation of doxorubicin-induced cytotoxicity incubated for 48 hrs by MTT assay
    [PMID: 36242992]
    NCI/ADR-RES EC50
    4.89 μM
    Compound: VRP
    Inhibition of P-gp in human MCF7/ADR cells assessed as reversal of multidrug resistance at 10 uM by measuring EC50 for adriamycin-induced cytotoxicity after 48 hrs by SRB colorimetric assay
    Inhibition of P-gp in human MCF7/ADR cells assessed as reversal of multidrug resistance at 10 uM by measuring EC50 for adriamycin-induced cytotoxicity after 48 hrs by SRB colorimetric assay
    [PMID: 25856545]
    NCI/ADR-RES IC50
    78.08 μM
    Compound: VRP
    Cytotoxicity against human MCF7/ADR cells after 48 hrs by MTT assay
    Cytotoxicity against human MCF7/ADR cells after 48 hrs by MTT assay
    [PMID: 29407947]
    NCI-H292 IC50
    0.18 μM
    Compound: Verapamil
    Potentiation of gefitinib-induced cytotoxicity against human NCI-H292 cells assessed as gefitinib IC50 at 50 uM after 72 hrs by SRB assay
    Potentiation of gefitinib-induced cytotoxicity against human NCI-H292 cells assessed as gefitinib IC50 at 50 uM after 72 hrs by SRB assay
    [PMID: 25215856]
    NCI-H292 IC50
    1.2 μM
    Compound: Verapamil
    Potentiation of erlotinib-induced cytotoxicity against human NCI-H292 cells assessed as erlotinib IC50 at 50 uM after 72 hrs by SRB assay
    Potentiation of erlotinib-induced cytotoxicity against human NCI-H292 cells assessed as erlotinib IC50 at 50 uM after 72 hrs by SRB assay
    [PMID: 25215856]
    NCI-H460 IC50
    10.3 μM
    Compound: Verapamil
    Potentiation of erlotinib-induced cytotoxicity against human H460 cells assessed as erlotinib IC50 at 50 uM after 72 hrs by SRB assay
    Potentiation of erlotinib-induced cytotoxicity against human H460 cells assessed as erlotinib IC50 at 50 uM after 72 hrs by SRB assay
    [PMID: 25215856]
    NCI-H460 IC50
    19.6 μM
    Compound: Verapamil
    Potentiation of gefitinib-induced cytotoxicity against human H460 cells assessed as gefitinib IC50 at 50 uM after 72 hrs by SRB assay
    Potentiation of gefitinib-induced cytotoxicity against human H460 cells assessed as gefitinib IC50 at 50 uM after 72 hrs by SRB assay
    [PMID: 25215856]
    NCI-H69 EC50
    27.8 μM
    Compound: Verapamil
    Modulation of MRP1 mediated drug efflux in doxorubicin-resistant human H69 cells assessed as accumulation of calcein AM incubated for 15 mins prior to calcein AM addition measured after 30 mins by fluorescence analysis
    Modulation of MRP1 mediated drug efflux in doxorubicin-resistant human H69 cells assessed as accumulation of calcein AM incubated for 15 mins prior to calcein AM addition measured after 30 mins by fluorescence analysis
    [PMID: 25311564]
    NIH3T3 CC50
    > 60 μM
    Compound: VRP
    Intrinsic cytotoxicity against mouse NIH/3T3 cells transfected with human MDR1 by MTT assay
    Intrinsic cytotoxicity against mouse NIH/3T3 cells transfected with human MDR1 by MTT assay
    [PMID: 26836364]
    NIH3T3 CC50
    27 μM
    Compound: VRP
    Intrinsic cytotoxicity against mouse NIH/3T3 cells by MTT assay
    Intrinsic cytotoxicity against mouse NIH/3T3 cells by MTT assay
    [PMID: 26836364]
    Oocyte IC50
    30 μM
    Compound: Verapamil
    Inhibition of chloroquine-resistant Plasmodium falciparum Dd2 CRT expressed in Xenopus laevis oocytes assessed as reduction in [3H]-chloroquine uptake after 1.5 to 2 hrs
    Inhibition of chloroquine-resistant Plasmodium falciparum Dd2 CRT expressed in Xenopus laevis oocytes assessed as reduction in [3H]-chloroquine uptake after 1.5 to 2 hrs
    [PMID: 23145816]
    Oocyte IC50
    30 μM
    Compound: 2
    Inhibition of chloroquine-resistant Plasmodium falciparum D10 CRT expressed in Xenopus laevis oocytes assessed as [3H]-chloroquine uptake after 1 to 2 hrs
    Inhibition of chloroquine-resistant Plasmodium falciparum D10 CRT expressed in Xenopus laevis oocytes assessed as [3H]-chloroquine uptake after 1 to 2 hrs
    [PMID: 21396749]
    P388 IC50
    3.1 μM
    Compound: Verapamil
    Multidrug-resistant reversal activity using P388/VMDRC.04 cells (a subline of P388 murine leukemia cells expressing human recombinant human P-glycoprotein) in the presence of 10 nM vincristine
    Multidrug-resistant reversal activity using P388/VMDRC.04 cells (a subline of P388 murine leukemia cells expressing human recombinant human P-glycoprotein) in the presence of 10 nM vincristine
    [PMID: 10386932]
    P388 IC50
    53 μM
    Compound: Verapamil
    Evaluated for cytotoxicity using P388/VMDRC.04 cells (a subline of P388 murine leukemia cells expressing human recombinant human P-glycoprotein) in the absence of 10 nM vincristine
    Evaluated for cytotoxicity using P388/VMDRC.04 cells (a subline of P388 murine leukemia cells expressing human recombinant human P-glycoprotein) in the absence of 10 nM vincristine
    [PMID: 10386932]
    PBMC IC50
    116.6 μM
    Compound: VP
    Cytotoxicity against human PBMC assessed as cell viability after 3 days by AlamarBlue assay
    Cytotoxicity against human PBMC assessed as cell viability after 3 days by AlamarBlue assay
    [PMID: 26197353]
    Splenocyte IC50
    55 μM
    Compound: Verapamil
    Cytotoxicity against C57BL/6J mouse splenocytes after 72 hrs by alamar blue assay
    Cytotoxicity against C57BL/6J mouse splenocytes after 72 hrs by alamar blue assay
    [PMID: 17846138]
    SW-620 IC50
    0.3 μM
    Compound: Verapamil
    Reversal of resistance to paclitaxel-induced cytotoxicity in human SW-620/AD300 cells assessed as reduction in paclitaxel IC50 at 4 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 4.23 +/- 0.50 uM)
    Reversal of resistance to paclitaxel-induced cytotoxicity in human SW-620/AD300 cells assessed as reduction in paclitaxel IC50 at 4 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 4.23 +/- 0.50 uM)
    [PMID: 34723530]
    SW-620 IC50
    7.11 μM
    Compound: Verapamil
    Reversal of resistance to paclitaxel-induced cytotoxicity in human SW-620 cells assessed as reduction in paclitaxel IC50 at 4 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 7.69 +/- 2.78 nM)
    Reversal of resistance to paclitaxel-induced cytotoxicity in human SW-620 cells assessed as reduction in paclitaxel IC50 at 4 uM preincubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 7.69 +/- 2.78 nM)
    [PMID: 34723530]
    SW-620 IC50
    7.11 μM
    Compound: VPM
    Reversal of resistance to paclitaxel-induced cytotoxicity against human SW620 cells by measuring paclitaxel IC50 at 4 uM pre-incubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 7.69 +/- 2.78 nM)
    Reversal of resistance to paclitaxel-induced cytotoxicity against human SW620 cells by measuring paclitaxel IC50 at 4 uM pre-incubated for 4 hrs followed by paclitaxel addition and measured after 72 hrs by MTT assay (Rvb = 7.69 +/- 2.78 nM)
    [PMID: 33280384]
    SW620/AD300 IC50
    > 30 μM
    Compound: Verapamil
    Antiproliferative activity against human SW620/AD300 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    Antiproliferative activity against human SW620/AD300 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    [PMID: 31975579]
    SW620/AD300 IC50
    0.81 μM
    Compound: Verapamil
    Reversal of P-gp mediated multidrug resistance in human SW620/AD300 cells assessed as potentiation of doxorubicin-induced antiproliferative activity by measuring doxorubicin IC50 at 2.5 uM after 48 hrs by MTT assay (Rvb = 4.9 microM)
    Reversal of P-gp mediated multidrug resistance in human SW620/AD300 cells assessed as potentiation of doxorubicin-induced antiproliferative activity by measuring doxorubicin IC50 at 2.5 uM after 48 hrs by MTT assay (Rvb = 4.9 microM)
    [PMID: 31975579]
    SW620/AD300 IC50
    2.98 μM
    Compound: VRP
    Reversal of Pgp-mediated DOX resistance in human SW620/AD300 cells assessed as potentiation of DOX-induced cytotoxicity by measuring DOX IC50 at 1 uM incubated for 48 hrs by SRB assay (Rvb = 33.39 +/- 7.08 uM)
    Reversal of Pgp-mediated DOX resistance in human SW620/AD300 cells assessed as potentiation of DOX-induced cytotoxicity by measuring DOX IC50 at 1 uM incubated for 48 hrs by SRB assay (Rvb = 33.39 +/- 7.08 uM)
    [PMID: 32329342]
    THP-1 IC50
    19.1 μM
    Compound: VER
    Antileishmanial activity against wild-type Leishmania amazonensis MHOM/BR/1973/MM2269 promastigotes infected in human THP1 cells by luciferase based assay
    Antileishmanial activity against wild-type Leishmania amazonensis MHOM/BR/1973/MM2269 promastigotes infected in human THP1 cells by luciferase based assay
    [PMID: 17452480]
    THP-1 IC50
    40.3 μM
    Compound: VER
    Antileishmanial activity against wild-type Leishmania major LV39 promastigotes infected in human THP1 cells by luciferase based assay
    Antileishmanial activity against wild-type Leishmania major LV39 promastigotes infected in human THP1 cells by luciferase based assay
    [PMID: 17452480]
    THP-1 IC50
    43.2 μM
    Compound: VER
    Antileishmanial activity against wild-type Leishmania infantum MHOM/MA/67/ITMAP-263 promastigotes infected in human THP1 cells by luciferase based assay
    Antileishmanial activity against wild-type Leishmania infantum MHOM/MA/67/ITMAP-263 promastigotes infected in human THP1 cells by luciferase based assay
    [PMID: 17452480]
    Ventricular myocyte IC50
    0.1 μM
    Compound: Verapamil
    Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
    Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
    [PMID: 22761000]
    Ventricular myocyte IC50
    0.164 μM
    Compound: Verapamil
    Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
    Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
    [PMID: 22761000]
    Ventricular myocyte IC50
    0.6 μM
    Compound: Verapamil
    Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
    Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
    [PMID: 22761000]
    Ventricular myocyte IC50
    0.79 μM
    Compound: Verapamil
    Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
    Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
    [PMID: 22761000]
    Ventricular myocyte IC50
    0.94 μM
    Compound: Verapamil
    Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
    Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
    [PMID: 22761000]
    Ventricular myocyte IC50
    100 nM
    Compound: Verapamil
    Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes
    Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes
    [PMID: 21300721]
    Vero IC50
    57.3 μg/mL
    Compound: verapamil
    Cytotoxicity against african green monkey Vero cells assessed as reduction in cell viability by MTT assay
    Cytotoxicity against african green monkey Vero cells assessed as reduction in cell viability by MTT assay
    [PMID: 25238443]
    In Vitro

    The EverFluor FL Verapamil (EFV) uptake by TR-iBRB2 cells is inhibited by cationic drugs, and inhibits by verapamil in a concentration-dependent manner with an IC50 of 98.0 μM[4].

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

    In Vivo

    Given orally Verapamil is useful for the prophylaxis of atrioventricular reentry tachycardia, and also in modulating the atrioventricular nodal response in atrial fibrillation[2].
    Verapamil is injected i.v. into a femoral vein prior to ischemia. Verapamil (1 mg/kg) significantly decreases the incidence of ventricular arrhythmias including premature ventricular contractions (PVC), ventricular tachycardia (VT) and ventricular fibrillation (VF) for 45-min coronary artery occlusion. Total arrhythmia scores are significantly increased when the heart is subjected to ischemia. Verapamil (1 mg/kg) significantly prevents the enhancement of total arrhythmia scores induced by ischemia[5].

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

    Clinical Trial
    Molecular Weight

    454.60

    Formula

    C27H38N2O4

    CAS No.
    Appearance

    Oil

    Color

    Colorless to light yellow

    SMILES

    COC1=CC=C(C(C#N)(C(C)C)CCCN(CCC2=CC=C(OC)C(OC)=C2)C)C=C1OC

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (219.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1997 mL 10.9987 mL 21.9974 mL
    5 mM 0.4399 mL 2.1997 mL 4.3995 mL
    View the 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.96%

    References

    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 (protect from light). 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 1 mM 2.1997 mL 10.9987 mL 21.9974 mL 54.9934 mL
    5 mM 0.4399 mL 2.1997 mL 4.3995 mL 10.9987 mL
    10 mM 0.2200 mL 1.0999 mL 2.1997 mL 5.4993 mL
    15 mM 0.1466 mL 0.7332 mL 1.4665 mL 3.6662 mL
    20 mM 0.1100 mL 0.5499 mL 1.0999 mL 2.7497 mL
    25 mM 0.0880 mL 0.4399 mL 0.8799 mL 2.1997 mL
    30 mM 0.0733 mL 0.3666 mL 0.7332 mL 1.8331 mL
    40 mM 0.0550 mL 0.2750 mL 0.5499 mL 1.3748 mL
    50 mM 0.0440 mL 0.2200 mL 0.4399 mL 1.0999 mL
    60 mM 0.0367 mL 0.1833 mL 0.3666 mL 0.9166 mL
    80 mM 0.0275 mL 0.1375 mL 0.2750 mL 0.6874 mL
    100 mM 0.0220 mL 0.1100 mL 0.2200 mL 0.5499 mL
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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