| 货号 | 2012/50 |
| 别名 | (8R)-8-Ethyl-1,4,7,8-tetrahydro-4-5 |
| 供应商 | Tocris |
| 生物活性 | Potent and selective antagonist for the human adenosine A3 receptor, with low affinity for the rat A3 receptor (Ki values are 2.3 and > 10000 nM respectively). Displays > 1000-fold selectivity over human A1 and A2A receptors (Ki values are 4.1 and 3.3 μM respectively) and > 180-fold selectivity over rat A1, rat A2A and mouse A2B receptors. Acts as an inverse agonist in the [35S]GTPγS binding assay in hA3-CHO cells (IC50 = 36 nM). |
| 运输条件 | Blue Ice |
| 存放说明 | 4℃ |
| 纯度 | >98 % |
| 计算分子量 | 331.8 |
| 分子式 | C16H17N5O.HCl |
| 可溶性/溶解性 | Soluble to 20 mM in DMSO with gentle warming |
| CAS号 | 444717-56-0 |
| 参考文献 | Muller (2003) Medicinal chemistry of adenosine A3 receptor ligands. Curr.Top.Med.Chem. 3 445. PMID: 12570761. Ozolaet al (2003) 2-Phenylimidazo[2,1-i]purin-5-ones: structure-activity relationships and characterization of potent and selective inverse agonists at human A3 adenosine receptors. Bioorg.Med.Chem. 11 347. PMID: 12517430. Mulleret al (2002) Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A2A- and A3-adenosine receptor antagonists. J.Med.Chem. 45 3440. PMID: 12139454. |