Biological Activity
Potent neuropeptide Y (NPY) Y5 receptor antagonist (Ki = 1.5 nM in vitro). Displays ≥ 3300-fold affinity for Y5 over Y1, Y2 and Y4 receptors. Also binds human 5-HT2B and 5-HT1A receptors (Ki values are 247 and 478 nM respectively). Exerts anxiolytic- and antidepressant-like effects in rat models of stress sensitivity.
Technical Data
| M. Wt | 423.62 |
| Formula | C19H25N3O2S3 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 304008-29-5 |
| PubChem ID | 22254068 |
| InChI Key | UWSBTSAJZMIHBL-UHFFFAOYSA-N |
| Smiles | O=S(NC[C@H](CC4)CC[C@@H]4NC1=NC(C2=CC=CC=C2SCC3)=C3S1)(C)=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 | 42.36 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 423.62. 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 | 2.36 mL | 11.8 mL | 23.61 mL |
| 5 mM | 0.47 mL | 2.36 mL | 4.72 mL |
| 10 mM | 0.24 mL | 1.18 mL | 2.36 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.47 mL |
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References
References are publications that support the products' biological activity.
Walker et al (2009) The novel neuropeptide Y Y5 receptor antagonist Lu AA33810 [N-[[trans-4-[(4,5-dihydro[1]benzothiepino[5,4-d]thiazol-2-yl)amino]cyclohexyl]methyl]-methanesulfonamide] exerts anxiolytic- and antidepressant-like effects J.Pharmacol.Exp.Ther. 328 900 PMID: 19098165
Keywords: LU AA33810, supplier, LUAA33810, potent, NPY, neuropeptide, Y, receptors, Y5, antagonists, neuropeptides, NPY, Receptors, NPY, Receptors, Tocris Bioscience
