| 货号 | 3621/50 |
| 别名 | (S)-1-(2-Amino-2-carboxyethyl)-3-(2 |
| 供应商 | Tocris |
| 生物活性 | GLUK5 kainate receptor antagonist (IC50 = 130 nM); also blocks recombinant homomeric GLUK7 receptors. Displays 12,700-fold selectivity for GLUK5 over GLUK6. Exhibits no activity at mGlu group I or NMDA receptors at concentrations of up to 10 μM. Apparent KD value is 18 ± 4 nM for depression of kainate responses on the dorsal root. |
| 运输条件 | Blue Ice |
| 存放说明 | 4℃ |
| 纯度 | >98 % |
| 计算分子量 | 353.35 |
| 分子式 | C14H15N3O6S |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO |
| 参考文献 | Perraiset al (2009) Antagonism of recombinant and native GluK3-containing kainate receptors. Neuropharmacology 56 131. PMID: 18761361. Dolmanet al (2007) Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: Role of the substituent at the 5-position of the uracil ring in development of highly potent and selective GLUK5 kainate receptor antagonists. J.Med.Chem. 50 1558. PMID: 17348638. Mayeret al (2006) Crystal structures of the kainate receptor GluR5 ligand binding core dimer with novel GluR5-selective antagonists. J.Neurosci. 26 2852. PMID: 16540562. |