Biological Activity
Potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively). Inhibits ADL-orexin B-mediated locomotion following i.p. administration in vivo and blocks orexin-A (Cat.No.1455) mediated increases in feeding behaviour. Brain penetrant.
Licensing Information
Manufactured and sold under license from Merck & Co., Inc. for use solely for preclinical research purposes (ie: not for administration to or other use in humans)
Technical Data
| M. Wt | 470.59 |
| Formula | C27H26N4O2S |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 916141-36-1 |
| PubChem ID | 11960895 |
| InChI Key | YSBGRVXJEMSEQY-DEOSSOPVSA-N |
| Smiles | O=C(CSC2=NC(C=CC=C5)=C5N2C)N1CCC[C@H]1[C@](NC3=CC=CC=C3C4=CC=CC=C4)=O |
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 | 47.06 | 100 | |
| ethanol | 47.06 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 470.59. 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 | 2.12 mL | 10.62 mL | 21.25 mL |
| 5 mM | 0.42 mL | 2.12 mL | 4.25 mL |
| 10 mM | 0.21 mL | 1.06 mL | 2.12 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Winrow et al (2010) Orexin receptor antagonism prevents transcriptional and behavioral plasticity resulting from stimulant exposure. Neuropharmacology 58 185 PMID: 19596018
Bergman et al (2008) Proline bis-amides as potent dual orexin receptor antagonists. Bioorg.Med.Chem.Letts 18 1425 PMID:
Khoo et al (2017) The dual orexin receptor antagonist TCS1102 does not affect reinstatement of nicotine-seeking. PLoS One 12 PMID: 28296947
Keywords: TCS 1102, supplier, TCS1102, orexin, receptors, OX1, OX2, antagonists, non-selective, dual, potent, merck, Non-selective, Orexin, Non-selective, Orexin, Tocris Bioscience
