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
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.

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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.

All Tocris products are intended for laboratory research use only.

Solubility Data

SolubilitySoluble to 100 mM in DMSO and to 100 mM in ethanol

Preparing Stock Solutions

The following data is based on the product molecular weight 484.18. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.07 mL 10.33 mL 20.65 mL
5 mM 0.41 mL 2.07 mL 4.13 mL
10 mM 0.21 mL 1.03 mL 2.07 mL
50 mM 0.04 mL 0.21 mL 0.41 mL

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Product Datasheets

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References

References are publications that support the products' biological activity.

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, supplier, JNJ10397049, Orexins, hypocretins, receptors, antagonists, selective, OX2R, OX2, sleep, OX2, Receptor, OX2, Receptor, Tocris Bioscience

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