货号 | 5613/50 |
别名 | 3-Fluoro-5-[3-(5-fluoro-2-pyridinyl |
供应商 | Tocris |
生物活性 | Potent and selective mGlu5 antagonist (IC50 values are 2.6 and 7.6 nM for rat and human receptors, respectively). Exhibits >3900-fold selectivity for mGlu5 over other mGlu receptors. Also selective over a panel of other targets. Displays discriminative effects in rats. Orally bioavailable and brain penetrant. |
运输条件 | Blue Ice |
存放说明 | Ambient |
纯度 | >98 % |
计算分子量 | 284.22 |
分子式 | C14H6F2N4 |
可溶性/溶解性 | Soluble to 50 mM in DMSO |
参考文献 | Swedberg and Raboisson (2014) AZD9272 and AZD2066: selective and highly central nervous system penetrant mGluR5 antagonists characterized by their discriminative effects. J.Pharmacol.Exp.Ther. 350 212. PMID: 24876235. Raboissonet al (2012) Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. Bioorg.Med.Chem.Lett. 22 6974. PMID: 23046966. |