RP 67580

Name: RP 67580
Brand: Tocris Bioscience
SKU: 1635

Tocris Bioscience, part of Bio-Techne | Catalog # 1635

Citations (80)

COA / SDS

Potent and selective NK1 antagonist

Key Product Details

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)
Molecular Weight:	438.57

View Full Technical Details for RP 67580

Technical Data
Citations

Biological Activity for RP 67580

RP 67580 is a potent and selective tachykinin NK₁ receptor antagonist (K_i 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 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	11.40 mL	22.80 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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References for RP 67580

References are publications that support the biological activity of the product.

Rupniak Antinociceptive activity of NK₁ receptor antagonists: non-specific effects of racemic RP67580. Br.J.Pharmacol. 1993 PMID: 8306108
Fong Molecular basis for the species selectivity of the neurokinin-1 receptor antagonists CP-96,345 and RP67580. J.Biol.Chem. 1992 PMID: 1281470
Garret Pharmacological properties of a potent and selective nonpeptide substance P antagonist. Proc.Natl.Acad.Sci.U.S.A. 1991 PMID: 1719549
Beaujouan Higher potency of RP 67580, in the mouse and the rat compared with other nonpeptide and peptide tachykinin NK₁ antagonists. Br.J.Pharmacol. 1993 PMID: 7682138