Regadenoson
(Synonyms: 瑞加德松; CVT-3146) 目录号 : GC13082
A short-acting A2A receptor agonist
Cas No.:313348-27-5
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
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:
[1] Cerqueira MD. The future of pharmacologic stress: selective A2A adenosine receptor agonists. Am J Cardiol. 2004 Jul 22;94(2A):33D-40D; discussion 40D-42D.
| Cas No. | 313348-27-5 | SDF | |
| 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°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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5618 mL | 12.809 mL | 25.618 mL |
| 5 mM | 0.5124 mL | 2.5618 mL | 5.1236 mL |
| 10 mM | 0.2562 mL | 1.2809 mL | 2.5618 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。