JNJ 10397049

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Cat.No. 4317 - JNJ 10397049 | C19H20Br2N2O3 | CAS No. 708275-58-5
Description: Selective OX2 receptor antagonist
Chemical Name: N-(2,4-Dibromophenyl)-N'-[(4S,5S)-2,2-dimethyl-4-phenyl-1,3-dioxan-5-yl]-urea
Purity: ≥99% (HPLC)
Datasheet
Citations (1)
Reviews
Literature

Biological Activity

Selective OX2 receptor antagonist (pIC50 = 7.4 for chimeric OX2 receptors; pKB values are 5.9 and 8.5 for OX1 and OX2 receptors respectively). Shows no significant activity in a panel of over 50 other neurotransmitters and neuropeptide receptors. Achieves high level of OX2 receptor occupancy in the rat brain; exhibits sleep-promoting effects in rats.

Compound Libraries

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Technical Data

M. Wt 484.18
Formula C19H20Br2N2O3
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 708275-58-5
PubChem ID 9869934
InChI Key RBKIJGLHFFQHBE-IRXDYDNUSA-N
Smiles O=C(N[C@@H]2[C@H](C3=CC=CC=C3)OC(C)(C)OC2)NC1=C(Br)C=C(Br)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solubility Soluble to 100 mM in DMSO and to 100 mM in ethanol

References

References are publications that support the biological activity of the product.

Dugovic et al (2009) Blockade of orexin-1 receptors attenuates orexin-2 receptor antagonism-induced sleep promotion in the rat. J.Pharmacol.Exp.Ther. 330 142 PMID: 19363060

Tran et al (2011) Chimeric, mutant orexin receptors show key interactions between orexin receptors, peptides and antagonists. Eur.J.Pharmacol. 667 120 PMID: 21679703

Gozzi et al (2011) Functional magnetic resonance imaging reveals different neural substrates for the effects of orexin-1 and orexin-2 receptor antagonists. PLoS ONE 6 e16406 PMID: 21307957


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Keywords: JNJ 10397049, JNJ 10397049 supplier, JNJ10397049, Orexins, hypocretins, receptors, antagonists, selective, OX2R, OX2, sleep, Receptor, 4317, Tocris Bioscience

1 Citation for JNJ 10397049

Citations are publications that use Tocris products. Selected citations for JNJ 10397049 include:

Mavanji et al (2015) Promotion of Wakefulness and Energy Expenditure by Orexin-A in the Ventrolateral Preoptic Area. Sleep 38 1361 PMID: 25845696


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