Verapamil hydrochloride
Chemical Name: α-[3-[[2-(3,4-Dimethoxyphenyl)ethyl]methylamino]propyl]-3,4-dimethoxy-α-(1-methylethyl)benzeneacetonitrile hydrochloride
Purity: ≥99%
Biological Activity
Verapamil hydrochloride is an L-type calcium channel blocker, anti-arrythmic, vasodilator and adrenergic antagonist. Induces autophagy by modulating cellular metabolism. Verapamil is a P-glycoprotein inhibitor and can reverse resistance to glucocorticoids and cancer treatments. Verapamil has been identified as targeting human host proteins that interact with SARS-CoV-2.Scientific Data
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Pluripotent stem cell-derived cardiomyocytes secrete Pro-BNP in response to small molecule-induction of cardiac hypertrophy. Cardiomyocytes were treated with the vasoconstrictor, ET-1 (Endothelin-1; Catalog # 1160), or one of two L-type calcium channel inhibitors, Doxorubicin (Catalog # 2252) or Verapamil (Catalog # 0654). Levels of the cardiac hypertrophy marker, Pro-Brain Natriuretic Peptide (Pro-BNP), were detected via Luminex® bead-based multiplex assay (Catalog # LXSAH). A substantial increase in Pro-BNP was detected in the medium of cardiomyocytes treated with ET-1, a known inducer of cardiac hypertrophy. Conversely, Doxorubicin and Verapamil decreased Pro-BNP secretion from cardiomyocytes.
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Verapamil affects cardiomyocyte contraction rates. The effect of small molecules on cardiomyocyte contraction rate was assessed by monitoring intracellular calcium fluctuations, where an increase in calcium coincides with cardiomyocyte contraction. Cardiomyocytes were loaded with the fluorescent calcium indicator, Fluo-4, prior to small molecule treatment. Individual wells were first monitored for baseline rates of calcium fluctuation represented as beats per minute (bpm). Verapamil (10uM or 30uM, Catalog # 0654), an L-type calcium channel blocker, decreased the rate of calcium fluctuations in cardiomyocytes in a dose-dependent manner.
Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Chemical modulators of autophagy as biological probes and potential therapeutics.
Fleming et al.
Nat.Chem.Biol., 2011;7:9 -
Block of P-type Ca2+ channels in freshly dissociated rat cerebellar Purkinje neurons by dilt. and vera.
Ishibashi et al.
Brain Res., 1995;695:88 -
Interaction of RO-40-5967 and vera. with the stably expressed α1-subunit of the cardiac L-type calcium channel.
Lacinova et al.
J.Pharmacol.Exp.Ther., 1995;274:54 -
Effects of vera. on intimal thickening and vascular reactivity in the collared carotid artery of the rabbit.
Ustunes et al.
Br.J.Pharmacol., 1996;118:1681 -
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Gordon et al.
Nature, 2020;
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Citations for Verapamil hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for Verapamil hydrochloride include:
11 Citations: Showing 1 - 10
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An Automated Platform for Assessment of Congenital and Drug-Induced Arrhythmia with hiPSC-Derived Cardiomyocytes.
Authors: McKeithan Et al.
Front Physiol 2017;8:766
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Calcium-regulatory proteins as modulators of chemotherapy in human neuroblastoma.
Authors: Florea Et al.
Oncotarget 2017;8:22876
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Chemerin-induced arterial contraction is Gi- and calcium-dependent.
Authors: Ferland Et al.
Vascul Pharmacol 2017;88:30
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Ion Fluxes through KCa2 (SK) and Cav1 (L-type) Channels Contribute to Chronoselectivity of Adenosine A1 Receptor-Mediated Actions in Spontaneously Beating Rat Atria.
Authors: Bragança Et al.
Front Pharmacol 2016;7:45
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Binding of αherpesvirus Glycoprotein H to Surface α4β1-Integrins Activates Calcium-Signaling Pathways and Induces Phosphatidylserine Exposure on the Plasma Membrane.
Authors: Azab Et al.
FEMS Immunol Med Microbiol 2015;6
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Dissecting out the complex Ca2+-mediated phenylephrine-induced contractions of mouse aortic segments.
Authors: Fransen Et al.
Cereb Cortex 2015;10:e0121634
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Optimisation of embryonic and larval ECG measurement in zebrafish for quantifying the effect of QT prolonging drugs.
Authors: Dhillon Et al.
PLoS One 2013;8:e60552
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Areca nut-induced buccal mucosa fibroblast contraction and its signaling: a potential role in oral submucous fibrosis--a precancer condition.
Authors: Chang Et al.
PLoS One 2013;34:1096
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Identification of quaternary ammonium compounds as potent inhibitors of hERG potassium channels.
Authors: Xia Et al.
Toxicol Appl Pharmacol 2011;252:250
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Calcium homeostasis and cone signaling are regulated by interactions between calcium stores and plasma membrane ion channels.
Authors: Szikra Et al.
PLoS One 2009;4:e6723
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Efficient intracellular multiplication of Legionella pneumophila in human monocytes requires functional host cell L-type calcium channels.
Authors: Wieland Et al.
Carcinogenesis 2006;47:296
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