| 货号 | 2010/50 |
| 别名 | 8-Ethyl-1,4,7,8-tetrahydro-4-methyl |
| 供应商 | Tocris |
| 生物活性 | Potent and highly selective antagonist for the human adenosine A3 receptor, with low affinity for the rat A3 receptor (Ki values are 0.44 and > 17000 nM respectively). Displays > 3800-fold selectivity over human A1, A2A and A2B receptors (Ki values are 4.1, 3.3 and 30 μM respectively) and > 1800-fold selectivity over rat A1 and A2A receptors. Acts as an inverse agonist in the [35S]GTPγS binding assay in hA3-CHO cells (IC50 = 4 nM). Produces thermal hyperalgesia in mice in vivo. |
| 运输条件 | Blue Ice |
| 存放说明 | 4℃ |
| 纯度 | >98 % |
| 计算分子量 | 435.14 |
| 分子式 | C16H14Cl3N5O.HCl |
| 可溶性/溶解性 | Soluble to 25 mM in DMSO and to 10 mM in ethanol |
| CAS号 | 591771-91-4 |
| 参考文献 | Abo-Salemet al (2004) Antinociceptive effects of novel A2B adenosine receptor antagonists. J.Pharmacol.Exp.Ther. 308 358. PMID: 14563788. 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. |