VUF 8430 dihydrobromide

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Cat.No. 2494 - VUF 8430 dihydrobromide | C4H11N5S.2HBr | CAS No. 100130-32-3
Description: Potent, high affinity H4 agonist
Chemical Name: 2-[(Aminoiminomethyl)amino]ethyl carbamimidothioic acid ester dihydrobromide
Datasheet
Citations (1)
Literature

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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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


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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


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