GR 203040

Pricing Availability Delivery Time Qty
Cat.No. 4647 - GR 203040 | C20H24N6O.2HCl | CAS No. 168398-02-5
Description: Potent, selective NK1 receptor antagonist
Chemical Name: (2S,3S)-N-[[2-Methoxy-5-(1H-tetrazol-1-yl)phenyl]methyl]-2-phenyl-3-piperidinamine dihydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

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

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 437.37. Batch specific molecular weights may vary from batch to batch due to solvent 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 2.29 mL 11.43 mL 22.86 mL
5 mM 0.46 mL 2.29 mL 4.57 mL
10 mM 0.23 mL 1.14 mL 2.29 mL
50 mM 0.05 mL 0.23 mL 0.46 mL

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Product Datasheets

Safety Datasheet

References

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


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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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