Verapamil 是一种钙通道阻滞剂,是一种口服有效的 P-gp 抑制剂。Verapamil 抑制 CYP3A4,可用于治疗高血压、心律失常和心绞痛的研究。
产品描述
Verapamil is a calcium channel blocker and an orally active and effective inhibitor of P-gp. Verapamil inhibits CYP3A4 and can be used in studies about the treatment of high blood pressure, heart arrhythmias, and angina research.
体外活性
Verapamil inhibits the EverFluor FL Verapamil (EFV) uptake by TR-iBRB2 cells with an IC50 of 98.0 μM in a concentration-dependent manner[1].
体内活性
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[3]. Verapamil(oral) is useful for the prophylaxis of atrioventricular reentry tachycardia, and also in modulating the atrioventricular nodal response in atrial fibrillation[4].
Cas No.
52-53-9
分子式
C27H38N2O4
分子量
454.6
别名
(±)-Verapamil;维拉帕米;CP-16533-1;NSC 135784
储存和溶解度
DMSO:Soluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years