Biological Activity
Potent and selective neuropeptide Y Y5 receptor antagonist (IC50 values are 3.1, >10000, >10000 and >10000 nM for Y5, Y1, Y2 and Y4 receptors respectively). Does not block NPY-induced feeding in vivo. Orally active and brain penetrant.
Compound Libraries
NPY 5RA972 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 351.44 |
| Formula | C21H25N3O2 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 439861-56-0 |
| PubChem ID | 9884833 |
| InChI Key | ZNFMHLDBJPAFEQ-UHFFFAOYSA-N |
| Smiles | CC1=C(NC(N4CCOCC4)=O)C=CC3=C1C2=CC=CC=C2N3C(C)C |
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 | 35.14 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 351.44. 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 | 2.85 mL | 14.23 mL | 28.45 mL |
| 5 mM | 0.57 mL | 2.85 mL | 5.69 mL |
| 10 mM | 0.28 mL | 1.42 mL | 2.85 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.57 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Block et al (2002) Discovery and optimization of a series of carbazole ureas as NPY5 antagonists for the treatment of obesity. J.Med.Chem. 45 3509 PMID: 12139462
Turnbull et al (2002) Selective antagonism of the NPY Y5 receptor does not have a major effect on feeding in rats. Diabetes 51 2441 PMID: 12145156
Morris et al (2007) Neuropeptide Y suppresses absence seizures in a genetic model primarily through effects on Y receptors. Eur.J.Neurosci. 25 1136 PMID: 17331209
Keywords: NPY 5RA972, supplier, NPY5RA972, neuropeptide, Y, Y5, receptors, antagonists, potent, selective, NPYY5, neuropeptides, NPY, Receptors, NPY, Receptors, Tocris Bioscience
