| 货号 | 4558/50 |
| 别名 | N-Ethyl-2-[(6-methoxy-3-pyridinyl)[ |
| 供应商 | Tocris |
| 生物活性 | Highly potent, selective OX2 receptor antagonist (IC50 values are 2.3 nM and 1900 nM for OX2 and OX1 respectively). Displays negligible or no inhibition of a panel of 80 receptors. Blocks orexin-B- and orexin-A-invoked calcium mobilization in hOX2-expressing CHO cells (IC50 values are 7.9 nM and 8.8 nM respectively); reverses orexin-B-induced hyperlocomotion in mice. Brain penetrant. |
| 运输条件 | Blue Ice |
| 存放说明 | -20℃ |
| 纯度 | >98 % |
| 计算分子量 | 454.54 |
| 分子式 | C23H26N4O4 |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO and to 100 mM in ethanol |
| 参考文献 | Mochizukiet al (2011) Orexin receptor 2 expression in the posterior hypothalamus rescues sleepiness in narcoleptic mice. Proc.Natl.Acad.Sci.U.S.A 108 4471. PMID: 21368172. Malherbeet al (2010) Mapping the binding pocket of dual antagonist almorexant to human orexin 1 and orexin 2 receptors: comparison with the selective OX1 antagonist SB-674042 and the selective OX2 antagonist N-ethyl-2-[(6-methoxy-pyridin-3-yl)-(toluene-2-sulfonyl)-amino]-N-pyridin-3-ylmethyl-acetamide (EMPA). Mol.Pharmacol. 78 81. PMID: 20404073. Malherbeet al (2009) Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX2 receptor. Br.J.Pharmacol. 156 1326. PMID: 19751316. |