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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)
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 Data 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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Product Datasheets for GR 203040
References for GR 203040
References are publications that support the biological activity of the product.
Beattie et al (1995) The pharmacology of GR203040, a novel, potent and selective non-peptide tachykinin NK1 receptor antagonist. Br.J.Pharmacol. 116 3149 PMID: 8719789
Gardner et al (1995) The broad-spectrum anti-emetic activity of the novel non-peptide tachykinin NK1 receptor antagonist GR203040. Br.J.Pharmacol. 116 3158 PMID: 8719790
Ward et al (1995) 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. 38 4985 PMID: 8544174
If you know of a relevant reference for GR 203040, please let us know.
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Keywords: GR 203040, GR 203040 supplier, GR203040, potent, selective, tachykinin, NK1, receptor, antagonists, antagonism, antiemetics, Receptor, 4647, Tocris Bioscience
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