Biological Activity
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.
Compound Libraries
Proxyfan oxalate is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 306.32 |
| Formula | C13H16N2O.C2H2O4 |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 177708-09-7 |
| PubChem ID | 76900838 |
| InChI Key | QVMZCQMJBQSPSW-UHFFFAOYSA-N |
| Smiles | OC(=O)C(O)=O.C(COCC1=CC=CC=C1)CC1=CN=CN1 |
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 | 33.24 | 100 | |
| water | 33.23 | 100 |
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 |
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Product Datasheets
References
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
Gbahou et al (2003) Protean agonism at histamine H3 receptors in vitro and in vivo. Proc.Natl.Acad.Sci.USA 100 11086 PMID:
Keywords: Proxyfan oxalate, supplier, High, affinity, H3, ligands, Receptors, Histamine, histaminergic, Histamine, H3, Receptors, Histamine, H3, Receptors, Tocris Bioscience
