RP 67580

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Cat.No. 1635 - RP 67580 | C29H30N2O2 | CAS No. 135911-02-3
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)
Datasheet
Citations (4)
Literature

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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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


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Keywords: RP 67580, supplier, Potent, selective, NK1, antagonists, Tachykinin, Receptors, Neurokinin, RP67580, NK1, Receptor, NK1, Receptor, 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

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

Wang et al (2008) TRPV1-mediated protection against endotoxin-induced hypotension and mortality in rats. J Neurosci 294 R1517 PMID: 18337316


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