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Submit ReviewRP 67580
Description: Potent and selective NK1 antagonist
Chemical Name: (3aR,7aR)-Octahydro-2-[1-imino-2-(2-methoxyphenyl)ethyl]-7,7-diphenyl-4H-isoindol
Purity: ≥97% (HPLC)
Biological Activity for RP 67580
RP 67580 is a 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.
Compound Libraries for RP 67580
RP 67580 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for RP 67580
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for RP 67580
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| ethanol | 43.86 | 100 | |
| DMSO | 21.93 | 50 |
Preparing Stock Solutions for RP 67580
The following data is based on the product molecular weight 438.57. Batch specific molecular weights may vary from batch to batch due to the degree 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 for RP 67580
References for RP 67580
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for RP 67580, please let us know.
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Keywords: RP 67580, RP 67580 supplier, Potent, selective, NK1, antagonists, Tachykinin, Receptors, Neurokinin, RP67580, Receptor, 1635, Tocris Bioscience
4 Citations for RP 67580
Citations are publications that use Tocris products. Selected citations for RP 67580 include:
Russell et al (2012) Activation of PAR(2) receptors sensitizes primary afferents and causes leukocyte rolling and adherence in the rat knee joint. Br J Pharmacol 167 1665 PMID: 22849826
Wang et al (2014) Innervation of enteric mast cells by primary spinal afferents in guinea pig and human small intestine. Am J Physiol Gastrointest Liver Physiol 307 G719 PMID: 25147231
Wang et al (2008) TRPV1-mediated protection against endotoxin-induced hypotension and mortality in rats. J Neurosci 294 R1517 PMID: 18337316
Zhong and Wang (2009) Protease-activated receptor 2-mediated protection of myocardial ischemia-reperfusion injury: role of transient receptor potential vanilloid receptors. Am J Physiol Regul Integr Comp Physiol 297 R1681 PMID: 19812353
Do you know of a great paper that uses RP 67580 from Tocris? Please let us know.
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Literature in this Area
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