Biological Activity
Potent and selective tachykinin NK1 receptor antagonist (Ki values are 2.9 nM and > 10 μM for rat NK1, and rat NK2 and NK3 receptors respectively). Displays higher affinity at rat and mouse than human receptors. Antinociceptive in vivo, possibly partly via inhibition of calcium channels.
Technical Data
| M. Wt | 438.57 |
| Formula | C29H30N2O2 |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 135911-02-3 |
| PubChem ID | 107686 |
| InChI Key | VWBOQFANCXZMAU-LOSJGSFVSA-N |
| Smiles | [H][C@@]13[C@@](CN(C(CC4=C(OC)C=CC=C4)=N)C3)([H])C(CCC(C5=CC=CC=C5)1C2=CC=CC=C2)=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 | 21.93 | 50 | |
| ethanol | 43.86 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 438.57. 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 | 2.28 mL | 11.4 mL | 22.8 mL |
| 5 mM | 0.46 mL | 2.28 mL | 4.56 mL |
| 10 mM | 0.23 mL | 1.14 mL | 2.28 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Beaujouan et al (1993) Higher potency of RP 67580, in the mouse and the rat compared with other nonpeptide and peptide tachykinin NK1 antagonists. Br.J.Pharmacol. 108 793 PMID: 7682138
Fong et al (1992) Molecular basis for the species selectivity of the neurokinin-1 receptor antagonists CP-96,345 and RP67580. J.Biol.Chem. 267 25668 PMID: 1281470
Garret et al (1991) Pharmacological properties of a potent and selective nonpeptide substance P antagonist. Proc.Natl.Acad.Sci.U.S.A. 88 10208 PMID: 1719549
Rupniak et al (1993) Antinociceptive activity of NK1 receptor antagonists: non-specific effects of racemic RP67580. Br.J.Pharmacol. 110 1607 PMID: 8306108
Keywords: RP 67580, supplier, Potent, selective, NK1, antagonists, Tachykinin, Receptors, Neurokinin, RP67580, NK1, Receptor, NK1, Receptor, Tocris Bioscience
