- Vesnarinone
-
- $48.00 / 5mg
-
2026-04-22
- CAS:81840-15-5
- Min. Order:
- Purity: 98.75%
- Supply Ability: 10g
|
| | VESNARINONE Basic information |
| Product Name: | VESNARINONE | | Synonyms: | 3，4-Dihydro-6-[4-(3，4-dimethoxybenzoyl)-1-piperazinyl]-2(1H)-quinolinone;VESNARINONE;Arkin;Piteranometozine;OPC 8212;6-[4-(3,4-Dimethoxybenzoyl)-1-piperazinyl]-3,4-dihydro-2(1H)-quinolinone;0PC-8212;Vesnarinone(OPC8212) | | CAS: | 81840-15-5 | | MF: | C22H25N3O4 | | MW: | 395.45 | | EINECS: | | | Product Categories: | | | Mol File: | 81840-15-5.mol |  |
| | VESNARINONE Chemical Properties |
| Melting point | 238.1-239.5° (Tominaga); mp 238.1-239.8° (Shimizu) | | Boiling point | 519.41°C (rough estimate) | | density | 1.2414 (rough estimate) | | refractive index | 1.6500 (estimate) | | storage temp. | Store at -20°C | | solubility | DMSO:9.84(Max Conc. mg/mL);24.88(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);1.26(Max Conc. mM)
DMF:3.0(Max Conc. mg/mL);7.59(Max Conc. mM) | | form | A crystalline solid | | pka | 2.86(at 25℃) | | color | White to off-white |
| | VESNARINONE Usage And Synthesis |
| Description | Vesnarinone is a new orally-active positive inotropic agent introduced for the treatment
of congestive heart failure. It exerts a positive inotropic effect on the heart and has a peripheral vasodilatory effect. Vesnarinone is claimed not to affect heart rate or aggravate
arrhythmia. | | Description | Vesnarinone is an inhibitor of phosphodiesterase 3 (PDE3; IC50s = 10.7 and 13.2 μM for PDE3A and PDE3B, respectively). It also inhibits ether-a-go-go-related gene 1 (ERG1) channels (IC50 = 1.1 μM in HEK293T cells expressing human ERG1). Vesnarinone (3-300 μM) increases contractile tension in isolated ventricular muscles of dog, cat, rabbit, and guinea pig in a dose-dependent manner. 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. | | Chemical Properties | Colorless granular crystals from ethanol-chloroform, melting point 238.1-239.5°C; also odorless and tasteless light yellow crystalline powder, melting point 238.1-239.8°C. UV maximum absorption (methanol, ethanol, chloroform): 271 nm (ε25100, 25200, 23000, C=10μg/m1). Solubility % (25°C): glacial acetic acid 18.68, chloroform 14.19, benzyl alcohol 5.913, N-methyl-2-pyrrolidone 3.407, dimethyl sulfoxide 2.509, cyclobutanesulfone 1.229, dimethylformamide 1.179, dioxane 0.1653, methanol 0.1151, acetone 0.06389, ethanol 0.04005, water 0.002086. pKa 2.86. | | Originator | Otsuka (Japan) | | Uses | Cardiotonic. | | Definition | ChEBI: Arkin (TN) is an organic molecular entity. | | Brand name | Arkin (Otsuka America);Arkin-Z. | | References | [1] MOHSEN NIKPOUR . Design, synthesis and biological evaluation of 6-(benzyloxy)-4-methylquinolin-2(1H)-one derivatives as PDE3 inhibitors[J]. Bioorganic & Medicinal Chemistry, 2010, 18 2: Pages 855-862. DOI: 10.1016/j.bmc.2009.11.044
[2] Y KATAYAMA. Inhibitory effects of vesnarinone on cloned cardiac delayed rectifier K(+) channels expressed in a mammalian cell line.[J]. Journal of Pharmacology and Experimental Therapeutics, 2000, 294 1: 339-346.
[3] FELDMAN A M. Pharmacologic Properties and Clinical Evaluation of the New Inotropic Agent OPC-8212 (Vesnarinone)[J]. Cardiovascular Therapeutics, 1993, 11 1: 1-11. DOI: 10.1111/j.1527-3466.1993.tb00264.x
[4] MD S E R, FACC James B Y M Richard Holubkov PhD, FACC Jay N C M B G White PhD, et al. Estrogen is associated with improved survival in aging women with congestive heart failure: analysis of the vesnarinone studies[J]. Journal of the American College of Cardiology, 2000, 36 2: Pages 529-533. DOI: 10.1016/s0735-1097(00)00738-5 |
| | VESNARINONE Preparation Products And Raw materials |
|