VUF 8430 dihydrobromide
Cat. No. 2494
Chemical Name: 2-[(Aminoiminomethyl)amino]ethyl carbamimidothioic acid ester dihydrobromide
Biological ActivityHigh 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.
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.
Certificate of Analysis / Product Datasheet / Safety Datasheet
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.
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.
Sterk et al (1986) The influence of guanidio and isothiourea groups in histaminergic compounds on H2-activity. Agents Actions 18 137. PMID: 2942013.
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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.
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