Biological Activity
OX2 receptor antagonist. Exhibits approximately six-fold selectivity for OX2 versus OX1 receptors. Decreases activity and increases sleep time in mice during the active phase, without affecting REM/NREM balance. Orally bioavailable. Brain penetrant.
Technical Data
| M. Wt | 405.49 |
| Formula | C23H27N5O2 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1373765-19-5 |
| PubChem ID | 56970858 |
| InChI Key | PCMHOSYCWRRHTG-UHFFFAOYSA-N |
| Smiles | COC1=CC=NC(N2CCC3(C(N(CC4=CNC5=C4C=CC=C5)CCC3)=O)CC2)=N1 |
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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 40.55 | 100 | |
| DMSO | 40.55 | 100 | |
| ethanol | 20.27 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 405.49. 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 | 2.47 mL | 12.33 mL | 24.66 mL |
| 5 mM | 0.49 mL | 2.47 mL | 4.93 mL |
| 10 mM | 0.25 mL | 1.23 mL | 2.47 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.49 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Hoyer et al (2013) Distinct effects of IPSU and suvorexant on mouse sleep architecture. Front.Neurosci. 7 230 PMID: 24376396
Betschart et al (2013) Identification of a novel series of orexin receptor antagonists with a distinct effect on sleep architecture for the treatment of insomnia. J.Med.Chem. 56 7590 PMID: 23964859
Keywords: IPSU, supplier, OX2, receptors, antagonists, antagonism, orexins, sleep, orally, bioavailable, brain, penetrant, OX2, Receptor, OX2, Receptor, Tocris Bioscience
