| Bioactivity | JNJ-10397049 is a potent and selective orexin 2 receptor (OX2R) antagonist, with a pKi of 8.3. JNJ-10397049 is 600-fold selective for the OX2R over the OX1R[1][2]. | ||||||||||||
| In Vivo | JNJ-10397049 (10-30 mg/kg) decreases the latency for persistent sleep and increased nonrapid eye movement and rapid eye movement sleep time[2].JNJ-10397049 blocks ethanol self-administration, place preference and reinstatement[3]. Animal Model: | ||||||||||||
| Name | JNJ-10397049 | ||||||||||||
| CAS | 708275-58-5 | ||||||||||||
| Formula | C19H20Br2N2O3 | ||||||||||||
| Molar Mass | 484.18 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Laura C McAtee, et al. Novel substituted 4-phenyl-[1,3]dioxanes: potent and selective orexin receptor 2 (OX(2)R) antagonists. Bioorg Med Chem Lett. 2004 Aug 16;14(16):4225-9. [2]. Christine Dugovic, et al. Blockade of orexin-1 receptors attenuates orexin-2 receptor antagonism-induced sleep promotion in the rat. J Pharmacol Exp Ther. 2009 Jul;330(1):142-51. [3]. Da-Thao Tran, et al. Chimeric, mutant orexin receptors show key interactions between orexin receptors, peptides and antagonists. Eur J Pharmacol. 2011 Sep 30;667(1-3):120-8. |
JNJ-10397049
CAS: 708275-58-5 F: C19H20Br2N2O3 W: 484.18
JNJ-10397049 is a potent and selective orexin 2 receptor (OX2R) antagonist, with a pKi of 8.3. JNJ-10397049 is 600-fold
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