JNJ-10397049

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].

Product Specifications

CAS Number

[708275-58-5]

UNSPSC

12352005

Target

Orexin Receptor (OX Receptor)

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/jnj-10397049.html

Purity

99.19

Solubility

DMSO : 170 mg/mL (ultrasonic)

Smiles

BrC1=C(NC(N[C@@H]2[C@H](C3=CC=CC=C3)OC(C)(C)OC2)=O)C=CC(Br)=C1

Molecular Formula

C19H20Br2N2O3

Molecular Weight

484.18

References & Citations

[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.