Biological Activity
Selective non-peptide orexin OX1 receptor antagonist. pKb values are 7.2 and < 5 for inhibition of intracellular Ca2+ release in CHO cells expressing human OX1 and OX2 receptors respectively. Blocks orexin-A induced grooming and feeding following systemic administration in vivo.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
Compound Libraries
SB 334867 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 319.32 |
| Formula | C17H13N5O2 |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 792173-99-0 |
| PubChem ID | 6604926 |
| InChI Key | AKMNUCBQGHFICM-UHFFFAOYSA-N |
| Smiles | CC1=NC2=CC=C(NC(=O)NC3=CC=NC4=CC=CN=C34)C=C2O1 |
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 | 31.93 | 100mM with gentle warming | |
| ethanol | 3.19 | 10mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 319.32. 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 | 3.13 mL | 15.66 mL | 31.32 mL |
| 5 mM | 0.63 mL | 3.13 mL | 6.26 mL |
| 10 mM | 0.31 mL | 1.57 mL | 3.13 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.63 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Duxon et al (2001) Evidence that orexin-A-evoked grooming in the rat is mediated by orexin-1 (OX1) receptors, with downstream 5-HT2C receptor involvement. Psychopharmacology 153 203 PMID: 11205420
Haynes et al (2000) A selective orexin-1 receptor antagonist reduces food consumption in male and female rats. Regul.Pept. 96 45 PMID: 11102651
Porter et al (2001) 1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor. Bioorg.Med.Chem.Lett. 11 1907 PMID: 11459658
Smart et al (2001) SB-334867-A: the first selective orexin-1 receptor antagonist. Br.J.Pharmacol. 132 1179 PMID: 11250867
Keywords: SB 334867, supplier, Selective, non-peptide, OX1, antagonists, Orexin1, Receptors, SB334867, GlaxoSmithKline, GSK, OX1, Receptor, OX1, Receptor, Tocris Bioscience
