Biological Activity
Potent and selective orexin OX1 receptor antagonist (Kb values are 41 and 560 nM for OX1 and OX2 receptors respectively). Elicits anxiolytic effects in vivo. Brain penetrant and orally available.
Technical Data
| M. Wt | 518.64 |
| Formula | C31H38N2O5 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1354039-86-3 |
| PubChem ID | 54765113 |
| InChI Key | HXHOBPVRRPCTLG-SETSBSEESA-N |
| Smiles | O=C(NC(C)C)[C@@H]([C@]4=CC=CC=C4)N2CCC1=CC(OC)=C(OC)C=C1[C@@H]2CC3=CC(OC)=C(OC)C=C3 |
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 | |||
| DMSO | 51.86 | 100 | |
| ethanol | 51.86 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 518.64. 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 | 1.93 mL | 9.64 mL | 19.28 mL |
| 5 mM | 0.39 mL | 1.93 mL | 3.86 mL |
| 10 mM | 0.19 mL | 0.96 mL | 1.93 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.39 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Steiner et al (2013) Discovery and characterization of ACT-335827, an orally available, brain penetrant orexin receptor type 1 selective antagonist. ChemMedChem 8 898 PMID: 23589487
Keywords: ACT 335827, supplier, ACT335827, potent, selective, OX1, antagonists, orexin-1, orexin1, orally, available, brain, penetrant, receptors, OX1, Receptor, OX1, Receptor, Tocris Bioscience
