Catalog Number: 2494
Chemical Name: 2-[(Aminoiminomethyl)amino]ethyl carbamimidothioic acid ester dihydrobromide
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
  • Solubility:
    Soluble to 100 mM in water and to 100 mM in DMSO
  • Storage:
    Desiccate at RT
  • CAS No:
    100130-32-3
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.
Background References
  1. The influence of guanidio and isothiourea groups in histaminergic compounds on H2-activity.
    Sterk et al.
    Agents Actions, 1986;18:137
  2. Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist.
    Lim et al.
    J.Med.Chem., 2006;49:6650
  3. 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.
    Lim et al.
    J.Pharmacol.Exp.Ther., 2008;327:88
Citations:

The citations listed below are publications that use Tocris products. Selected citations for VUF 8430 dihydrobromide include:

1 Citations: Showing 1 - 1

  1. Enhancement of ionizing radiation response by histamine in vitro and in vivo in human breast cancer.
    Authors: Lamas Et al.
    Cancer Biol Ther 2014;16:137

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