| 货号 | 14139-1mg |
| 描述 | JNJ-10397049 is a potent, selective, and bioavailable antagonist of the orexin-2 receptor (OX2R) (KB = 4.5 nM for OX2R versus 1.1 µM for OX1R).1,2,3 It has no significant affinity for over 50 other neurotransmitters or neuropeptide receptors.1 Applied subcutaneously to rats, JNJ-10397049 decreases the latency to persistent sleep and increases persistent sleep time.1 This compound produces a widespread attenuation of D-amphetamine-induced relative cerebrovascular signal, with prominent cortical involvement, in rat brains assessed by functional magnetic resonance imaging.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Dugovic, C.,Shelton, J.E.,Aluisio, L.E., et al. Blockade of orexin-1 receptors attenuates orexin-2 receptor antagonism-induced sleep promotion in the rat. Journal of Pharmacology and Experimental Therapeutics 330(1), 142-151 (2009). 2.Faedo, S.,Perdonà, E.,Antolini, M., et al. Functional and binding kinetic studies make a distinction between OX1 and OX2 orexin receptor antagonists. European Journal of Pharmacology 692(1-3), 1-9 (2012). 3.Tran, D.T.,Bonaventure, P.,Hack, M., et al. Chimeric, mutant orexin receptors show key interactions between orexin receptors, peptides and antagonists. European Journal of Pharmacology 667(1-3), 120-128 (2011). 4.Gozzi, A.,Turrini, G.,Piccoli, L., et al. Functional magnetic resonance imaging reveals different neural substrates for the effects of orexin-1 and orexin-2 receptor antagonists. PLoS One 6(1), e16406 (2011). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 484.2 |
| 分子式 | C19H20Br2N2O3 |
| CAS号 | 708275-58-5 |
| 稳定性 | ≥ 2 years |
| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |