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| 品牌 | absin | CAS | 313348-27-5 |
|---|---|---|---|
| 分子式 | C15H18N8O5 | 纯度 | ＞98% |
| 分子量 | 390.35 | 货号 | abs47028126 |
| 规格 | 5mg | 供货周期 | 现货 |
| 主要用途 | is an adenosine derivative | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
Regadenoson 313348-27-5
| 产品描述 | |
| 描述 | Regadenoson is an adenosine derivative and selective A2A adenosine receptor agonist with coronary vasodilating activity. Upon administration, regadenoson selectively binds to and activates the A2A adenosine receptor, which induces coronary vasodilation. This leads to an increase in coronary blood flow and enhances myocardial perfusion. Compared to adenosine, regadenoson has a longer half-life and shows higher selectivity towards the A2A adenosine receptor. This agent is a very weak agonist for the A1 adenosine receptor and has negligible affinity for the A2B and A3 adenosine receptors. |
| 纯度 | ＞98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | 瑞加德松；CVT-3146 |
| 外观 | 白色至类白色粉末 |
| 可溶性/溶解性 | DMSO : 50 mg/mL (128.09 mM) |
| 生物活性 | |
| 靶点 | A2AR |
| In vitro(体外研究) | Regadenoson has a relatively low binding affinity (hA2A Ki=290 nM) for human A2A receptors and greater than 30-fold selectivity versus the A2B and A3AR subtypes and 13-fold over the A1AR. Regadenoson behaves as a weak partial agonist causing cAMP accumulation in PC12 cells but as a full and potent agonist causing coronary vasodilation. |
| In vivo(体内研究) | In a dog model, intravenous bolus injection of regadenoson causes a dose-dependent increase in myocardial blood flow and a dose-dependant decrease in coronary vascular resistance. In a rat heart model, regadenoson was shown to have a dose-dependent increase in heart rate and a decrease in mean arterial pressure at the higher doses. Regadenoson also caused more than a 2-fold increase in serum norepinephrine and epinephrine. For clinical data, Regadenoson has a volume of distribution of 11.5 L and 78.7 L (at steady-state), and an estimated clearance of 37.8 L/h. It is renally excreted (58% of total elimination) with a terminal half-life of 33 to 108 min. |
| 参考文献 | |
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| 研究领域 | |
| 研究领域 | Cardiovascular Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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