Verapamil
(Synonyms: 维拉帕米; (±)-Verapamil; CP-16533-1) 目录号 : GC61811
Verapamil是 L 型钙通道阻滞剂和肾上腺素能受体拮抗剂，常用于高血压、心律失常和心绞痛的研究。
Cas No.:52-53-9
Sample solution is provided at 25 µL, 10mM.
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Verapamil is an L-type calcium channel blocker and adrenergic receptor antagonist commonly used in studies of hypertension, arrhythmias and angina pectoris[1].
Verapamil (5µM-5mM; 1h) affects human erythrocytes, where the normal disc-like shape of the erythrocytes changes to oropharyngeal cysts, small cells, spherical oropharyngeal cysts and haemolysis occurs at a concentration of Verapamil of 5mM. As the concentration of Verapamil was increased from 5µM, the morphology of the erythrocytes changed [2].The survival and proliferation rates of PC-3, A549, and COLO 205 cells were decreased after treatment with Verapamil (50–200μM; 6–48h)[3] .
In the neuroinflammatory model, pretreatment with Verapamil (10mg/kg; ip; 7days) in the morning reduced CD11b+, CD68+ and Iba1 by 54.33%, 24.68% and 41.33%, respectively. The above markers were also reduced in evening pretreated mice by 41.01%, 18.3% and 24.06%, respectively [4].Long-term administration of Verapamil (200mg/kg; po; 10weeks) to mice rescued the lives of mice with myotonic dystrophy type 1 and improved myogenesis, muscle stiffness and respiratory function [5].Verapamil (1.0, 2.5, 5.0 and 10mg/kg; ip; 48h) impaired memory consolidation in a parameter- and dose-dependent manner in an absent-field habituation task in rats [6].
References:
[1] Kania E, Pająk B, O'Prey J, Sierra Gonzalez P, Litwiniuk A, Urbańska K, Ryan KM, Orzechowski A. Verapamil treatment induces cytoprotective autophagy by modulating cellular metabolism. FEBS J. 2017 May;284(9):1370-1387.
[2] Suwalsky M, Munoz M, Mennickent S, et al. Structural effects of verapamil on cell membranes and molecular models[J]. Journal of the Chilean Chemical Society, 2010, 55(1): 1-4.
[3] Mosalam EM, Elberri AI, Sallam AS, Salem HR, Metwally EM, Abdallah MS, Shaldam MA, Mansour HEA. Chronotherapeutic neuroprotective effect of verapamil against lipopolysaccharide-induced neuroinflammation in mice through modulation of calcium-dependent genes. Mol Med. 2022 Nov 26;28(1):139.
[4] Rattis BAC, Freitas AC, Oliveira JF, Calandrini-Lima JLA, Figueiredo MJ, Soave DF, Ramos SG, Celes MRN. Effect of Verapamil, an L-Type Calcium Channel Inhibitor, on Caveolin-3 Expression in Septic Mouse Hearts. Oxid Med Cell Longev. 2021 Apr 8;2021:6667074.
[5]Cisco LA, Sipple MT, Edwards KM, Thornton CA, Lueck JD. Verapamil mitigates chloride and calcium bi-channelopathy in a myotonic dystrophy mouse model. J Clin Invest. 2024 Jan 2;134(1):e173576.
[6]Popović N, Giménez de Béjar V, Caballero-Bleda M, Popović M. Verapamil Parameter- and Dose-Dependently Impairs Memory Consolidation in Open Field Habituation Task in Rats. Front Pharmacol. 2017 Jan 10;7:539.
Verapamil是 L 型钙通道阻滞剂和肾上腺素能受体拮抗剂，常用于高血压、心律失常和心绞痛的研究[1]。
Verapamil （5µM-5mM；1h）影响人红细胞，在在 5mM 浓度的Verapamil下，红细胞的正常圆盘状形状变为口咽囊肿、小细胞、球形口咽囊肿，并发生溶血。随着Verapamil浓度从 5µM 增加，红细胞的形态发生变化 [2]。PC-3、A549 和 COLO 205 细胞存活率和增殖率在Verapamil（50–200μM；6–48h）处理后降低 [3] 。
在神经炎症模型中，早晨给予Verapamil (10mg/kg；ip ；7天 ) 预处理分别使 CD11b+、CD68+ 和 Iba1 降低 54.33%、24.68% 和 41.33%，晚上预处理小鼠的以上标志物也有降低，分别降低了 41.01%、18.3% 和 24.06%[4]。小鼠长期服用Verapamil（200mg/kg； po； 10weeks）能挽救1型肌营养不良症小鼠的生命，并改善肌力生成、肌肉僵硬度和呼吸功能[5]。Verapamil (1.0、2.5、5.0和10 mg/kg；ip；48h)在大鼠的旷场习惯任务中以参数和剂量依赖性的方式损害记忆巩固[6]。
| Cell experiment [1]: | |
Cell lines | SHSY5Y cells |
Preparation Method | SHSY5Y cells were seeded into 24-well plates . 2% FBS medium containing Verapamil at a concentration range from 1nM to 0.5mM was added to the cells for 1, 6, 24 and 48h. Cell viability was assessed using the MTT reduction assay. |
Reaction Conditions | Verapamil: 1nM -0.5mM; 6, 24 and 348h. |
Applications | A highly statistical reduction in cell viability was observed under 0.5mM Verapamil treatment and was still not recovered after 48h; the other tested concentrations failed to produce any significant effects after 1, 6, and 24h. |
| Animal experiment [2]: | |
Animal models | Myotonic dystrophy mouse model |
Preparation Method | Mice were provided Verapamil via ingestion of Nutra-Gel Complete Nutrition food to a final dose of 200mg/kg/day Verapamil. Mice that did not receive verapamil, were provided Nutra-Gel Complete Nutrition food that had 1mL ddH2O added to serve as a vehicle control. |
Dosage form | Verapamil (200mg/kg; po; 10weeks) |
Applications | Long-term administration of the calcium channel blocker Verapamilto mice rescued the life of mice with myotonic dystrophy type 1 and improved force production, muscle stiffness, and respiratory function. |
References: | |
| Cas No. | 52-53-9 | SDF | |
| 别名 | 维拉帕米; (±)-Verapamil; CP-16533-1 | ||
| Canonical SMILES | COC1=CC=C(C(C#N)(C(C)C)CCCN(CCC2=CC=C(OC)C(OC)=C2)C)C=C1OC | ||
| 分子式 | C27H38N2O4 | 分子量 | 454.6 |
| 溶解度 | DMSO: 100 mg/mL (219.97 mM) | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1997 mL | 10.9987 mL | 21.9974 mL |
| 5 mM | 0.4399 mL | 2.1997 mL | 4.3995 mL |
| 10 mM | 0.22 mL | 1.0999 mL | 2.1997 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.50%
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