High affinity histamine H3 receptor ligand (pKi = 8.62) that acts as a protean agonist at recombinant and native receptors. In functional studies, activity ranges from full agonist to inverse agonist depending on system used. Displays partial agonist effects on cAMP inhibition and MAPK activity, neutral antagonist activity on histamine release and partial inverse agonism of [3H]-arachidonic acid release.
|Storage||Desiccate at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 306.32. 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||3.26 mL||16.32 mL||32.65 mL|
|5 mM||0.65 mL||3.26 mL||6.53 mL|
|10 mM||0.33 mL||1.63 mL||3.26 mL|
|50 mM||0.07 mL||0.33 mL||0.65 mL|
References are publications that support the products' biological activity.
Baldi et al (2005) The H3 receptor protean agonist proxyfan enhances the expression of fear memory in the rat. Neuropharmacology 48 246 PMID: 15695163
Krueger et al (2005) G protein-dependent pharmacology of histamine H3 receptor ligands: evidence for heterogeneous active state receptor conformations. J.Pharmacol.Exp.Ther 314 271 PMID: 15821027
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Keywords: Proxyfan oxalate, supplier, High, affinity, H3, ligands, Receptors, Histamine, histaminergic, Histamine, H3, Receptors, Histamine, H3, Receptors, Tocris Bioscience
1 Citation for Proxyfan oxalate
Citations are publications that use Tocris products. Selected citations for Proxyfan oxalate include:
Singh et al (2012) Development of time-resolved fluorescent based [EU]-GTP binding assay for selection of human Histamine 3 receptor antagonists/inverse agonist: a potential target for Alzheimer's treatment. Ann Neurosci 19 71 PMID: 25205969
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