GR 203040

Name: GR 203040
Brand: Tocris Bioscience
SKU: 4647

Tocris Bioscience, part of Bio-Techne | Catalog # 4647

Citations (1)

COA / SDS

Potent and selective NK1 antagonist

Key Product Details

Description:	Potent and selective NK₁ antagonist
Chemical Name:	(2S,3S)-N-[[2-Methoxy-5-(1H-tetrazol-1-yl)phenyl]methyl]-2-phenyl-3-piperidinamine dihydrochloride
Purity:	≥98% (HPLC)
Molecular Weight:	437.37

View Full Technical Details for GR 203040

Technical Data
Citations

Biological Activity for GR 203040

GR 203040 is a potent and selective NK₁ receptor antagonist. Potently inhibits substance P binding to NK₁ receptors (pKi = 10.1 to 10.5). Displays antiemetic activity in vivo.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Compound Libraries for GR 203040

GR 203040 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for GR 203040

M. Wt	437.37
Formula	C₂₀H₂₄N₆O.2HCl
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	168398-02-5
PubChem ID	127944
InChi Key	DZYPLFAASKBQBS-ICSRJNTNSA-N
Smiles	COC1=CC=C(N4N=NN=C4)C=C1CN[C@@H]2[C@H]([C@]3=CC=CC=C3)NCCC2.Cl.Cl

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 GR 203040

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	8.75	20
	DMSO	8.75	20

Preparing Stock Solutions for GR 203040

The following data is based on the product molecular weight 437.37.

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
0.2 mM	11.43 mL	57.16 mL	114.32 mL
1 mM	2.29 mL	11.43 mL	22.86 mL
2 mM	1.14 mL	5.72 mL	11.43 mL
10 mM	0.23 mL	1.14 mL	2.29 mL

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References for GR 203040

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

Gardner The broad-spectrum anti-emetic activity of the novel non-peptide tachykinin NK₁ receptor antagonist GR203040. Br.J.Pharmacol. 1995 PMID: 8719790
Ward Discovery of an orally bioavailable NK₁ receptor antagonist, (2S,3S)-(2-methoxy-5-tetrazol-1-ylbenzyl)(2-phenylpiperidin-3-yl)amine (GR203040), with potent antiemetic activity. J.Med.Chem. 1995 PMID: 8544174
Beattie The pharmacology of GR203040, a novel, potent and selective non-peptide tachykinin NK₁ receptor antagonist. Br.J.Pharmacol. 1995 PMID: 8719789