An oxrexin 2 receptor antagonist
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JNJ-10397049

Item No. 14139

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(2,4-dibromophenyl)-N'-[(4S,5S)-2,2-dimethyl-4-phenyl-1,3-dioxan-5-yl]-urea
CAS Number
708275-58-5
Molecular Formula
C19H20Br2N2O3
Formula Weight
484.2
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 50 mg/mlDMF:PBS (pH 7.2) (1:4): 0.2 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/ml
λmax
251 nm
SMILES
BrC1=CC(Br)=C(NC(N[C@@H]2[C@H](C3=CC=CC=C3)OC(C)(C)OC2)=O)C=C1
InChi Code
InChI=1S/C19H20Br2N2O3/c1-19(2)25-11-16(17(26-19)12-6-4-3-5-7-12)23-18(24)22-15-9-8-13(20)10-14(15)21/h3-10,16-17H,11H2,1-2H3,(H2,22,23,24)/t16-,17-/m0/s1
InChi Key
RBKIJGLHFFQHBE-IRXDYDNUSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    1 mg

    $54

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    5 mg

    $185

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    10 mg

    $262

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    Product Description

    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

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    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. J. Pharmacol. Exp. Ther. 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. Eur. J. Pharmacol. 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. Eur. J. Pharmacol. 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).