Vesnarinone (OPC-8212)
(Synonyms: 维司力农; OPC-8212) 目录号 : GC32110
A PDE3 inhibitor and ERG1 channel blocker
Cas No.:81840-15-5
Sample solution is provided at 25 µL, 10mM.
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Vesnarinone is an inhibitor of phosphodiesterase 3 (PDE3; IC50s = 10.7 and 13.2 μM for PDE3A and PDE3B, respectively).1 It also inhibits ether-a-go-go-related gene 1 (ERG1) channels (IC50 = 1.1 μM in HEK293T cells expressing human ERG1).2 Vesnarinone (3-300 μM) increases contractile tension in isolated ventricular muscles of dog, cat, rabbit, and guinea pig in a dose-dependent manner.3 Oral and i.v. administration of vesnarinone increases right ventricular pressure with no effect on heart rate in dog models of tricuspid insufficiency- and pulmonary stenosis-induced congestive heart failure. It also increases contractility and coronary flow while decreasing heart rate in a guinea pig model of aortic stenosis-induced congestive heart failure. Formulations containing vesnarinone have been used for the treatment of congestive heart failure.4
1.Nikpour, M., Sadeghian, H., Saberi, M.R., et al.Design, synthesis and biological evaluation of 6-(benzyloxy)-4-methylquinolin-2(1H)-one derivatives as PDE3 inhibitorsBioorg. Med. Chem.18(2)855-862(2010) 2.Katayama, Y., Fujita, A., Ohe, T., et al.Inhibitory effects of vesnarinone on cloned cardiac delayed rectifier K+ channels expressed in a mammalian cell lineJ. Pharmacol. Exp. Ther.294(1)339-346(2000) 3.Feldman, A.M.Pharmacologic properties and clinical evaluation of the new inotropic agent OPC-8212 (vesnarinone)Cardiovasc. Drug Rev.11(1)1-11(1993) 4.Reis, S.E., Holubkov, R., Young, J.B., et al.Estrogen is associated with improved survival in aging women with congestive heart failure: Analysis of the vesnarinone studiesJ. Am. Coll. Cardiol.36(2)529-533(2000)
| Cas No. | 81840-15-5 | SDF | |
| 别名 | 维司力农; OPC-8212 | ||
| Canonical SMILES | O=C1NC2=C(C=C(N3CCN(C(C4=CC=C(OC)C(OC)=C4)=O)CC3)C=C2)CC1 | ||
| 分子式 | C22H25N3O4 | 分子量 | 395.45 |
| 溶解度 | DMSO : 16.67 mg/mL (42.15 mM) | 储存条件 | Store at -20°C |
| 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 | 2.5288 mL | 12.6438 mL | 25.2876 mL |
| 5 mM | 0.5058 mL | 2.5288 mL | 5.0575 mL |
| 10 mM | 0.2529 mL | 1.2644 mL | 2.5288 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet