Verapamil HCl
(Synonyms: 盐酸维拉帕米; (±)-Verapamil hydrochloride; CP-16533-1 hydrochloride) 目录号 : GC17106
An L-type calcium channel blocker
Cas No.:152-11-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
myeloma cell lines (JK-6L, RPMI8226, and ARH-77 cell lines) |
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Preparation method |
The solubility of this compound in DMSO is >14.5mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
70 μM; 16 h |
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Applications |
In myeloma cell lines, the combination of bortezomib (10 nM) and verapamil (70 μM) markedly reduced the viability of the JK-6L, RPMI8226, and ARH-77 cell lines. JK-6L cells were more sensitive toward bortezomib and verapamil treatment. Combination of bortezomib and verapamil might induce predominantly apoptotic cell death and activation of caspase 3/7. |
| Animal experiment [2]: | |
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Animal models |
The collagen-induced arthritis (CIA) mice model |
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Dosage form |
20 mg/kg; intraperitoneally every day starting on day 21 |
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Application |
In CIA mice model, verapamil remarkably attenuated development of arthritis and alleviated inflammation. Verapamil also significantly reduced mRNA levels of inflammation-associated molecules, including IL-1β, IL-6, NOS-2, and COX-2. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Meister S1, 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 Jul;12(7):550-61. [2]. Wang W1, Li Z2, Meng Q3, et al. Chronic Calcium Channel Inhibitor Verapamil Antagonizes TNF-α-Mediated Inflammatory Reaction and Protects Against Inflammatory Arthritis in Mice. Inflammation. 2016 Oct;39(5):1624-34. |
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Verapamil hydrochloride is a calcium channel antagonist.
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[1]. The enzyme hydrolase activity of recombinant human carboxylesterase (CES2) is substantially inhibited by Verapamil with Ki of 3.84±0.99μM[2].
Verapamil, a calcium channel antagonist, 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 (P<0.01 vs. sham). Verapamil (1 mg/kg) significantly prevented the enhancement of total arrhythmia scores induced by ischemia (P<0.01 vs. ischemia). Results indicate that Verapamil exerts an anti-arrhythmic property[3].
References:
[1]. Meister S, 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.
[2]. Yanjiao X, et al. Evaluation of the inhibitory effects of antihypertensive drugs on human carboxylesterase in vitro. Drug Metab Pharmacokinet. 2013;28(6):468-74.
[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.
| Cas No. | 152-11-4 | SDF | |
| 别名 | 盐酸维拉帕米; (±)-Verapamil hydrochloride; CP-16533-1 hydrochloride | ||
| 化学名 | 2-(3,4-dimethoxyphenyl)-5-[2-(3,4-dimethoxyphenyl)ethyl-methylamino]-2-propan-2-ylpentanenitrile;hydrochloride | ||
| Canonical SMILES | CC(C)C(CCCN(C)CCC1=CC(=C(C=C1)OC)OC)(C#N)C2=CC(=C(C=C2)OC)OC.Cl | ||
| 分子式 | C27H39ClN2O4 | 分子量 | 491.06 |
| 溶解度 | ≥ 14.45mg/mL in DMSO, ≥ 8.95 mg/mL in EtOH with ultrasonic, ≥ 6.41 mg/mL in Water with ultrasonic | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.0364 mL | 10.1821 mL | 20.3641 mL |
| 5 mM | 0.4073 mL | 2.0364 mL | 4.0728 mL |
| 10 mM | 0.2036 mL | 1.0182 mL | 2.0364 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。