Biological Activity
Selective NPFF receptor antagonist (Ki values are 58 and 75 nM at hNPFF1 and hNPFF2 receptors respectively). Displays selectivity over several related receptors including NPY Y1 GPR10, GPR54, GPR103 and the opioid receptors. Blocks NPFF-induced hypothermia and increases in atrial blood pressure and heart rate, and prevents opioid-induced tolerance associated with hyperalgesia in vivo.
Technical Data
| M. Wt | 482.62 |
| Formula | C26H38N6O3 |
| Storage | Store at -20°C |
| CAS Number | 876310-60-0 |
| PubChem ID | 53320361 |
| InChI Key | UMKHUSRDQFQHAK-RNJMTYCLSA-N |
| Smiles | O=C(N[C@H]([C@](N[C@H](C(N)=O)CC4=CC=CC=C4)=O)CCCNC(N)=N)C1(CC(C3)C2)CC3CC2C1 |
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 | 4.83 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 482.62. 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 | 2.07 mL | 10.36 mL | 20.72 mL |
| 5 mM | 0.41 mL | 2.07 mL | 4.14 mL |
| 10 mM | 0.21 mL | 1.04 mL | 2.07 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.41 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Wang et al (2008) Neuropeptide FF receptors antagonist, RF9, attenuates opioid-evoked hypothermia in mice. Peptides 29 1183 PMID: 18406009
Simonin et al (2006) RF9, a potent and selective neuropeptide FF receptor antagonist, prevents opioid-induced tolerance associated with hyperalgesia. Proc.Natl.Acad.Sci.USA 103 466 PMID:
Fang et al (2008) Inhibition of neuropeptide FF (NPFF)-induced hypothermia and anti-morphine analgesia by RF9, a new selective NPFF receptors antagonist. Regul.Peptides 147 45 PMID:
Keywords: RF 9, supplier, Selective, NPFF1, NPFF2, antagonists, npffr1, npffr2, Neuropeptide, FF, AF, Receptors, FF/AF, RF9, neuropeptides, Neuropeptide, FF/AF, Receptors, Neuropeptide, FF/AF, Receptors, Tocris Bioscience
