GR 203040

Key Product Details

Product Description

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

Product Specifications for GR 203040

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

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

Product Documents for GR 203040