Verapamil

SKU: orb1306580

Description

Verapamil is an orally active, non-dihydropyridine calcium channel blocker that also inhibits P-glycoprotein and CYP3A4. It is widely used in research on hypertension, angina, and cardiac conditions, serving as a key pharmacological tool for in vitro and in vivo studies of calcium signaling and drug transport.

Research Area

Metabolism Research, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 52-53-9
• MW: 454.6016
• Purity: 99.96% (May vary between batches)
• Formula: C₂₇H₃₈N₂O₄
• SMILES: COC1=CC=C(CCN(C)CCCC(C#N)(C(C)C)C2=CC=C(OC)C(OC)=C2)C=C1OC
• Target: P-gp,Calcium Channel,Cytochromes P450
• Solubility: DMSO:45 mg/mL (98.99 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4.5 mg/mL (9.9 mM)

Bioactivity

• Target IC50:
  Kv1.5 channel:5.1 ± 0.5 μM (currents)|K+ channel (hERG):3.8 ± 0.2 μM (currents)|P-gp:1.1 μM (Ki)|Kv1.1 channel:14.0 ± 2.7 μM (currents)|Delayed outwardly rectifying K+ current:11 μM
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• In Vivo:
  Verapamil (1 mg/kg;i.v.) 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. Verapamil(oral) is useful for the prophylaxis of atrioventricular reentry tachycardia, and also in modulating the atrioventricular nodal response in atrial fibrillation.
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• In Vitro:
  Verapamil inhibits the EverFluor FL Verapamil (EFV) uptake by TR-iBRB2 cells with an IC50 of 98.0 μM in a concentration-dependent manner.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CP-16533-1, CYP3A4, CYPs, Cytochrome P450, Cluster of differentiation 243, CalciumChannel, CD243, ABCB1, (±)-Verapamil, angina, antiarrhythmic, Ca channels, Ca2+ channels, Calcium Channel, blood, inhibit, Multidrug resistance protein 1, NSC 135784, Palbociclib, lysosomotropic, NSC135784, NSC-135784, Inhibitor, high, MDR1, pressure, Pgp, P-gp, P-glycoprotein, Verapamil

Compound Identifiers

PubChem CID

2520