Biological Activity
High affinity (pKi = 7.5), potent histamine H4 receptor full agonist (pEC50 = 7.3). Displays moderate affinity for H3 receptors (pKi = 6.0) and weak partial agonist activity at H2 receptors.
Technical Data
| M. Wt | 323.05 |
| Formula | C4H11N5S.2HBr |
| Storage | Desiccate at RT |
| CAS Number | 100130-32-3 |
| PubChem ID | 3063227 |
| InChI Key | GPWJSTKHQMIXCA-UHFFFAOYSA-N |
| Smiles | Br.Br.NC(SCCNC(N)=N)=N |
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 | 32.31 | 100 | |
| water | 32.31 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 323.05. 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 | 3.1 mL | 15.48 mL | 30.95 mL |
| 5 mM | 0.62 mL | 3.1 mL | 6.19 mL |
| 10 mM | 0.31 mL | 1.55 mL | 3.1 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.62 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Sterk et al (1986) The influence of guanidio and isothiourea groups in histaminergic compounds on H2-activity. Agents Actions 18 137 PMID: 2942013
Lim et al (2006) Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist. J.Med.Chem. 49 6650 PMID: 17154494
Lim et al (2008) Phenylalanine 169 in the second extracellular loop of the human histamine H4 receptor is responsible for the difference in agonist binding between human and mouse H4 receptors. J.Pharmacol.Exp.Ther. 327 88 PMID: 18635748
Keywords: VUF 8430 dihydrobromide, supplier, Potent, high, affinity, H4, agonists, Receptors, Histamine, histaminergic, VUF8430, dihydrobromide, Histamine, H4, Receptors, Histamine, H4, Receptors, Tocris Bioscience
