GR 203040

Pricing Availability   Qty
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)
Literature (2)

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
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
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.

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

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

Citations for GR 203040

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Currently there are no citations for GR 203040. Do you know of a great paper that uses GR 203040 from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Peptides Involved in Appetite Modulation Scientific Review

Peptides Involved in Appetite Modulation Scientific Review

Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.

Depression Poster

Depression Poster

Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.