Biological Activity
Selective non-peptide orexin OX1 receptor antagonist (Kb values are 21.7 and 1405 nM for human OX1 and OX2 receptors respectively). Blocks orexin-A induced grooming following oral administration in vivo.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
Compound Libraries
SB 408124 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 356.37 |
| Formula | C19H18F2N4O |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 288150-92-5 |
| PubChem ID | 4331799 |
| InChI Key | JTARFZSNUAGHRB-UHFFFAOYSA-N |
| Smiles | CN(C)C1=CC=C(NC(=O)NC2=CC(C)=NC3=C(F)C=C(F)C=C23)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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 35.64 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 356.37. 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 | 2.81 mL | 14.03 mL | 28.06 mL |
| 5 mM | 0.56 mL | 2.81 mL | 5.61 mL |
| 10 mM | 0.28 mL | 1.4 mL | 2.81 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Langmead et al (2004) Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor. Br.J.Pharmacol. 141 340 PMID: 14691055
Porter (2001) Advances in novel 7-TM receptors: non-peptide orexin-1 antagonists. Royal Society of Chemistry Meeting. PMID:
Keywords: SB 408124, supplier, Selective, non-peptide, OX1, antagonists, Orexin1, Receptors, SB408124, GlaxoSmithKline, GSK, OX1, Receptor, OX1, Receptor, Tocris Bioscience
