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Verapamil HCl (Synonyms: NSC 272366, NSC 657799, (±)-Verapamil)

Catalog No.GC17106

Verapamil HCl ((±)-Verapamil HCl) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor.

Products are for research use only. Not for human use. We do not sell to patients.

Verapamil HCl Chemical Structure

Cas No.: 152-11-4

Size Price Stock Qty
10mM (in 1mL DMSO)
$41.00
In stock
1g
$49.00
In stock
5g
$128.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

myeloma cell lines (JK-6L, RPMI8226, and ARH-77 cell lines)

Preparation method

The solubility of this compound in DMSO is >14.5mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

70 μM; 16 h

Applications

In myeloma cell lines, the combination of bortezomib (10 nM) and verapamil (70 μM) markedly reduced the viability of the JK-6L, RPMI8226, and ARH-77 cell lines. JK-6L cells were more sensitive toward bortezomib and verapamil treatment. Combination of bortezomib and verapamil might induce predominantly apoptotic cell death and activation of caspase 3/7.

Animal experiment [2]:

Animal models

The collagen-induced arthritis (CIA) mice model

Dosage form

20 mg/kg; intraperitoneally every day starting on day 21

Application

In CIA mice model, verapamil remarkably attenuated development of arthritis and alleviated inflammation. Verapamil also significantly reduced mRNA levels of inflammation-associated molecules, including IL-1β, IL-6, NOS-2, and COX-2.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Meister S1, Frey B, Lang VR, et al. Calcium channel blocker verapamil enhances endoplasmic reticulum stress and cell death induced by proteasome inhibition in myeloma cells. Neoplasia. 2010 Jul;12(7):550-61.

[2]. Wang W1, Li Z2, Meng Q3, et al. Chronic Calcium Channel Inhibitor Verapamil Antagonizes TNF-α-Mediated Inflammatory Reaction and Protects Against Inflammatory Arthritis in Mice. Inflammation. 2016 Oct;39(5):1624-34.

Background

Verapamil hydrochloride is a calcium channel antagonist.

Verapamil (hydrochloride) is an L-type calcium channel antagonist. The combination of Bortezomib and Verapamil (70 µM) markedly declines the viability of the JK-6L, RPMI 8226, and ARH-77 cell lines after 16 hours of culture[1]. The enzyme hydrolase activity of recombinant human carboxylesterase (CES2) is substantially inhibited by Verapamil with Ki of 3.84±0.99μM[2].

Verapamil, a calcium channel antagonist, 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 (P<0.01 vs. sham). Verapamil (1 mg/kg) significantly prevented the enhancement of total arrhythmia scores induced by ischemia (P<0.01 vs. ischemia). Results indicate that Verapamil exerts an anti-arrhythmic property[3].

References:
[1]. Meister S, et al. Calcium channel blocker Verapamil enhances endoplasmic reticulum stress and cell death induced by proteasome inhibition in myeloma cells. Neoplasia. 2010 Jul;12(7):550-61.
[2]. Yanjiao X, et al. Evaluation of the inhibitory effects of antihypertensive drugs on human carboxylesterase in vitro. Drug Metab Pharmacokinet. 2013;28(6):468-74.
[3]. Zhou P, et al. Anti-arrhythmic effect of Verapamil is accompanied by preservation of cx43 protein in rat heart. PLoS One. 2013 Aug 12;8(8):e71567.

Chemical Properties

Cas No. 152-11-4 SDF
Synonyms NSC 272366, NSC 657799, (±)-Verapamil
Chemical Name 2-(3,4-dimethoxyphenyl)-5-[2-(3,4-dimethoxyphenyl)ethyl-methylamino]-2-propan-2-ylpentanenitrile;hydrochloride
Canonical SMILES CC(C)C(CCCN(C)CCC1=CC(=C(C=C1)OC)OC)(C#N)C2=CC(=C(C=C2)OC)OC.Cl
Formula C27H39ClN2O4 M.Wt 491.06
Solubility ≥ 14.45mg/mL in DMSO, ≥ 8.95 mg/mL in EtOH with ultrasonic, ≥ 6.41 mg/mL in Water with ultrasonic Storage 4°C, protect from light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.0364 mL 10.1821 mL 20.3641 mL
5 mM 0.4073 mL 2.0364 mL 4.0728 mL
10 mM 0.2036 mL 1.0182 mL 2.0364 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 34 reference(s) in Google Scholar.)

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