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Verapamil hydrochloride

MCE China：Verapamil hydrochloride

Brand：MedChemExpress (MCE)

Cat. No.HY-A0064

CAS：152-11-4

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

Purity：99.98%

Storage：4°C, sealed storage, away from moisture and light *In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light)

Shipping：Room temperature in continental US; may vary elsewhere.

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

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].

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].

Animal Administration：Rats[3] Adult male Sprague-Dawley (SD) rats (250−350 g) are used. Verapamil (1 mg/kg) is injected i.v. into a femoral vein 10 min prior to ischemia. A sham group undergoes the same surgical procedures, except the suture underneath the LAD is left untied. In another series of experiment, arrhythmia is induced by Bay K8644, an L-type calcium channel agonist, at a dose of 0.1 mg/kg given i.v. into the FV. Verapamil (1 mg/kg) is administered 10 min prior to Bay K8644. All injections are performed within 30 sec.

Cell Assay：Cells (1×105) are treated with 10 nM Bortezomib and/or 70 µM Verapamil for 16 hours and incubated for another 4 hours with Alamar-Blue. Activity of the mitochondrial dehydrogenase results in conversion of the coloring, which is followed by measurement of the absorption using a spectrophotometer[1].

IC50 & Target：CYP3

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References：

[1]. Gowarty JL, et al. Verapamil as a culprit of palbociclib toxicity. J Oncol Pharm Pract. 2019 Apr;25(3):743-746.  [Content Brief]

[2]. Krikler DM. Verapamil in arrhythmia. Br J Clin Pharmacol. 1986;21 Suppl 2:183S-189S.  [Content Brief]

[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.  [Content Brief]

[4]. Rehnqvist N,et al. Effects of metoprolol vs verapamil in patients with stable angina pectoris. The Angina Prognosis Study in Stockholm (APSIS). Eur Heart J. 1996 Jan;17(1):76-81.  [Content Brief]

[5]. Kubo Y, et al. Blood-to-Retina Transport of Fluorescence-Labeled Verapamil at the Blood-Retinal Barrier. Pharm Res. 2018 Mar 12;35(5):93.  [Content Brief]