| CAS NO: | 313348-27-5 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 50mg | 电议 |
| Cas No. | 313348-27-5 |
| 别名 | 瑞加德松; CVT-3146 |
| 化学名 | (Z)-1-(6-amino-9-((2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-9H-purin-2-yl)-N-methyl-1H-pyrazole-4-carbimidic acid |
| Canonical SMILES | C/N=C(O)/C(C=N1)=CN1C2=NC(N)=C(N=CN3[C@@]4([H])[C@@](O)([H])[C@@](O)([H])[C@@](O4)([H])CO)C3=N2 |
| 分子式 | C15H18N8O5 |
| 分子量 | 390.35 |
| 溶解度 | ≥ 18.05mg/mL in DMSO |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Description: Ki: 1095 nM for A2A receptor The adenosine A2A receptor is a G-protein-coupled receptor that has been extensively studied during the past few decades because it offers numerous possibilities for therapeutic applications. Regadenoson (CVT-3146) is a highly selective, potent, low affinity A2A adenosine agonist. In vitro: Regadenoson was selective for the A2A adenosine receptor versus the A1, A2B, and A3 receptors in binding and functional studies. Regadenoson was also found to be a full and potent agonist to cause coronary vasodilation, a response that has a very large A2A receptor reserve [1]. In vivo: In a study of 10 conscious dogs, authors compared intravenously injected regadenoson to that of adenosine. Regadenoson caused a dose-dependent increase of coronary blood flow (CBF), whereas adenosine was less potent but produced equivalent hyperemia. Thus, authors concluded that regadenoson is a potent coronary vasodilator with a short duration of action, minimal and transient systemic hemodynamic effects, and ease of administration [1]. Clinical trial: Previous study investigated the magnitude and duration of the effect of regadenoson on CBF velocity in humans. Results demonstrated that regadenoson produced a dose-dependent increase in duration of CBF velocity augmentation. At all dose levels, regadenoson caused a rapid increase in CBF velocity that was near peak within 30 seconds of the bolus delivery. Regadenoson was generally well tolerated, and side effects at all doses were infrequent, mild, and self-limited [1]. Reference: |
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