GR 125487 sulfamate

Name: GR 125487 sulfamate
Brand: Tocris Bioscience
SKU: 1658

Tocris Bioscience, part of Bio-Techne | Catalog # 1658

Citations (7)

COA / SDS

Potent and selective 5-HT4 antagonist; active in vivo

Key Product Details

Description:	Potent and selective 5-HT₄ antagonist; active in vivo
Chemical Name:	5-Fluoro-2-methoxy-[1-[2-[(methylsulfonyl)amino]ethyl]-4-piperidinyl]-1H-indole-3-methylcarboxylate sulfamate
Purity:	≥97% (HPLC)
Molecular Weight:	524.58

View Full Technical Details for GR 125487 sulfamate

Technical Data
Citations

Biological Activity for GR 125487 sulfamate

GR 125487 sulfamate is a potent and selective 5-HT₄ receptor antagonist (K_i = 0.19 nM for porcine 5-HT₄). Centrally active following systemic administration in vivo.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Technical Data for GR 125487 sulfamate

M. Wt	524.58
Formula	C₁₉H₂₆FN₃O₅S.H₂NSO₃H
Storage	Desiccate at RT
Purity	≥97% (HPLC)
CAS Number	859502-43-5
PubChem ID	6604955
InChi Key	VQJFDBXITIOGJM-UHFFFAOYSA-N
Smiles	NS(O)(=O)=O.COC1=C(C(=O)OCC2CCN(CCNS(C)(=O)=O)CC2)C2=CC(F)=CC=C2N1

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 for GR 125487 sulfamate

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	water	4.27	10 with gentle warming

Preparing Stock Solutions for GR 125487 sulfamate

The following data is based on the product molecular weight 524.58.

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
0.1 mM	19.06 mL	95.31 mL	190.63 mL
0.5 mM	3.81 mL	19.06 mL	38.13 mL
1 mM	1.91 mL	9.53 mL	19.06 mL
5 mM	0.38 mL	1.91 mL	3.81 mL

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References for GR 125487 sulfamate

References are publications that support the biological activity of the product.

Horikoshi Possible involvement of 5-HT₄ receptors, in addition to 5-HT₃ receptors, in the emesis induced by high-dose cisp. in Suncus murinus. Jpn.J.Pharmacol. 2001 PMID: 11243577
Schiavi Identification of serotonin 5-HT₄ recognition sites in the porcine caudate nucleus by radioligand binding. Neuropharmacology 1994 PMID: 7984293
Galeotti Role of 5-HT₄ receptors in the mouse passive avoidance test. J.Pharmacol.Exp.Ther. 1998 PMID: 9732367