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
JNJ 10397049 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
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
| Solubility | Soluble 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.
| 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 |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
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
Keywords: JNJ 10397049, supplier, JNJ10397049, Orexins, hypocretins, receptors, antagonists, selective, OX2R, OX2, sleep, OX2, Receptor, OX2, Receptor, Tocris Bioscience
