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Submit ReviewVUF 8430 dihydrobromide
Description: Potent and high affinity H4 agonist
Chemical Name: 2-[(Aminoiminomethyl)amino]ethyl carbamimidothioic acid ester dihydrobromide
Biological Activity for VUF 8430 dihydrobromide
VUF 8430 dihydrobromide is a 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 for VUF 8430 dihydrobromide
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for VUF 8430 dihydrobromide
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 32.31 | 100 | |
| DMSO | 32.31 | 100 |
Preparing Stock Solutions for VUF 8430 dihydrobromide
The following data is based on the product molecular weight 323.05. Batch specific molecular weights may vary from batch to batch due to the degree 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 for VUF 8430 dihydrobromide
References for VUF 8430 dihydrobromide
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for VUF 8430 dihydrobromide, please let us know.
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Keywords: VUF 8430 dihydrobromide, VUF 8430 dihydrobromide supplier, Potent, high, affinity, H4, agonists, Receptors, Histamine, histaminergic, VUF8430, dihydrobromide, 2494, Tocris Bioscience
1 Citation for VUF 8430 dihydrobromide
Citations are publications that use Tocris products. Selected citations for VUF 8430 dihydrobromide include:
Lamas et al (2014) Enhancement of ionizing radiation response by histamine in vitro and in vivo in human breast cancer. Cancer Biol Ther 16 137 PMID: 25482934
Do you know of a great paper that uses VUF 8430 dihydrobromide from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Histamine Receptors Scientific Review
Written by Iwan de Esch and Rob Leurs, this review provides a synopsis of the different histamine receptor subtypes and the ligands that act upon them; compounds available from Tocris are listed.