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Verapamil HCl

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Chemical Structure| 152-11-4 同义名 : CP-16533-1 hydrochloride;Verapamil (hydrochloride);NSC 657799;NSC 272366;(±)-Verapamil;CP-16533-1;Verapamil HCl;(±)-Verapamil hydrochloride
CAS号 : 152-11-4
货号 : A724474
分子式 : C27H39ClN2O4
纯度 : 99%
分子量 : 491.063
MDL号 : -
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(61.09 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(101.82 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • Calcium Channel
描述 Verapamil hydrochloride, a prototype calcium antagonist, is now marketed in the United States for the acute treatment of supraventricular tachyarrhythmias and for chronic management of vasospastic and chronic stable angina. It inhibits the slow inward channel in in the heart and blocks calcium influx in smooth muscle[3]. 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[4]. The enzyme hydrolase activity of recombinant human carboxylesterase (CES2) is substantially inhibited by Verapamil with Ki of 3.84±0.99μM[5]. 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. Verapamil may confer an anti-arrhythmic effect via calcium influx inhibition, inhibition of oxygen consumption and accompanied by preservation of Cx43 protein[6]. Combined fractional CO2 laser and topical 5-FU (5-fluorouracil) or verapamil hydrochloride offer a safe therapy for HTSs (hypertrophic scars) and keloids[7].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
A2780 cells Function assay Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay, IC50=4.57088 μM 18678495
Caco-2 cells Function assay Inhibition of Pgp measured as inhibition of [3H]vinblastine basolateral to apical transport in Caco-2 cells, EC50=20 μM 17064079
CCRF-CEM cells 5 μM Function assay The effective dose was measured against P-glycoprotein expressing CCRF-CEM cells in the presence of 5 uM daunomycin, ED50=0.045 μM 7629817
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.04mL

0.41mL

0.20mL

10.18mL

2.04mL

1.02mL

20.36mL

4.07mL

2.04mL
参考文献

[1]Yanjiao X, Chengliang Z, et al. Evaluation of the inhibitory effects of antihypertensive drugs on human carboxylesterase in vitro. Drug Metab Pharmacokinet. 2013;28(6):468-74.

[2]Meister S, Frey B, 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.

[3]Baky SH, Singh BN. Verapamil hydrochloride: pharmacological properties and role in cardiovascular therapeutics. Pharmacotherapy. 1982;2(6):328‐353

[4]Meister S, 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;12(7):550‐561

[5]Yanjiao X, Chengliang Z, Xiping L, Tao W, Xiuhua R, Dong L. Evaluation of the inhibitory effects of antihypertensive drugs on human carboxylesterase in vitro. Drug Metab Pharmacokinet. 2013;28(6):468‐474

[6]Zhou P, Zhang SM, Wang QL, Wu Q, Chen M, Pei JM. Anti-arrhythmic effect of verapamil is accompanied by preservation of cx43 protein in rat heart. PLoS One. 2013;8(8):e71567. Published 2013 Aug 12

[7]Sabry HH, Abdel Rahman SH, Hussein MS, Sanad RR, Abd El Azez TA. The Efficacy of Combining Fractional Carbon Dioxide Laser With Verapamil Hydrochloride or 5-Fluorouracil in the Treatment of Hypertrophic Scars and Keloids: A Clinical and Immunohistochemical Study. Dermatol Surg. 2019;45(4):536‐546