Biological Activity
Selective histamine H4 receptor agonist; displays 50-fold selectivity for the rat H4 receptor over the H3 subtype (pKi values are 5.75 and 7.46 for rat H3 and H4 receptors respectively). Also exhibits affinity for the human H4 receptor (pKi = 8.22).
Compound Libraries
VUF 10460 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 269.34 |
| Formula | C15H19N5 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1028327-66-3 |
| PubChem ID | 25129523 |
| InChI Key | NIJGWJIOMPHDBP-UHFFFAOYSA-N |
| Smiles | NC1=NC(C2=CC=CC=C2)=CC(N3CCN(C)CC3)=N1 |
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 | |||
| 2eq.HCl | 26.93 | 100 | |
| DMSO | 26.93 | 100 | |
| ethanol | 26.93 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 269.34. 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 | 3.71 mL | 18.56 mL | 37.13 mL |
| 5 mM | 0.74 mL | 3.71 mL | 7.43 mL |
| 10 mM | 0.37 mL | 1.86 mL | 3.71 mL |
| 50 mM | 0.07 mL | 0.37 mL | 0.74 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Altenbach et al (2008) Structure-activity studies on a series of a 2-aminopyrimidine-containing histamine H4 receptor ligands. J.Med.Chem. 51 6571 PMID: 18811133
Cowart et al (2008) Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models. J.Med.Chem. 51 6547 PMID: 18817367
Coruzzi et al (2011) Selective histamine H3 and H4 receptor agonists exert opposite effects against the gastric lesions induced by HCl in the rat stomach. Eur.J.Pharmacol. 669 121 PMID: 21839070
Keywords: VUF 10460, supplier, VUF10460, histamine, histaminergic, H4, receptors, agonists, selective, Histamine, H4, Receptors, Histamine, H4, Receptors, Tocris Bioscience
