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

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Product Description
Licensing Information
Product Specifications
Solubility
Preparing Stock Solutions
Calculators
Background References
Product Documents
Specific Notices

Key Product Details

Description

Potent and selective NK1 antagonist

View all NK1 Receptor Antagonists »

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

Molecular Weight

437.37

Formula

C₂₀H₂₄N₆O.2HCl

Storage

Store at -20°C

Purity

≥98% (HPLC)

Chemical Name

(2S,3S)-N-[[2-Methoxy-5-(1H-tetrazol-1-yl)phenyl]methyl]-2-phenyl-3-piperidinamine dihydrochloride

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.

Solubility

	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 all 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

Calculators

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Dilution Calculator

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Reconstitution Calculator

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