GR 125487 sulfamate

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Cat.No. 1658 - GR 125487 sulfamate | C19H26FN3O5S.H2NSO3H | CAS No. 859502-43-5
Description: Potent, 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)
Datasheet
Citations (2)
Literature

Biological Activity

Potent and selective 5-HT4 receptor antagonist (Ki = 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

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 4.27 10mM with gentle warming
phosphate buffered saline 2.14 5mM with gentle warming

Preparing Stock Solutions

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

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.91 mL 9.53 mL 19.06 mL
5 mM 0.38 mL 1.91 mL 3.81 mL
10 mM 0.19 mL 0.95 mL 1.91 mL
50 mM 0.04 mL 0.19 mL 0.38 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Galeotti et al (1998) Role of 5-HT4 receptors in the mouse passive avoidance test. J.Pharmacol.Exp.Ther. 286 1115 PMID: 9732367

Horikoshi et al (2001) Possible involvement of 5-HT4 receptors, in addition to 5-HT3 receptors, in the emesis induced by high-dose cisplatin in Suncus murinus. Jpn.J.Pharmacol. 85 70 PMID: 11243577

Schiavi et al (1994) Identification of serotonin 5-HT4 recognition sites in the porcine caudate nucleus by radioligand binding. Neuropharmacology 33 543 PMID: 7984293


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Keywords: GR 125487 sulfamate, supplier, Potent, selective, 5-HT4, antagonists, Serotonin, Receptors, 5-Hydroxytryptamine, GR125487, sulfamate, GlaxoSmithKline, GSK, 5-HT4, Receptors, Tocris Bioscience

2 Citations for GR 125487 sulfamate

Citations are publications that use Tocris products. Selected citations for GR 125487 sulfamate include:

Warner-Schmidt et al (2009) Role of p11 in cellular and behavioral effects of 5-HT4 receptor stimulation. Dis Model Mech 29 1937 PMID: 19211900

Orr et al (2015) Astrocytic adenosine receptor A2A and Gs-coupled signaling regulate memory. J Neurosci 18 423 PMID: 25622143


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