Clobenpropit dihydrobromide

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Cat.No. 0752 - Clobenpropit dihydrobromide | C14H17ClN4S.2HBr | CAS No. 145231-35-2
Description: Highly potent H3 antagonist and H4 partial agonist
Alternative Names: VUF 9153
Chemical Name: N-(4-Chlorobenzyl)-S-[3-(4(5)-imidazolyl)propyl]isothiourea dihydrobromide
Purity: ≥99% (HPLC)
Datasheet
Citations (3)
Literature

Biological Activity

An extremely potent histamine H3 antagonist/inverse agonist (pA2=9.93). Also displays partial agonist activity at H4 receptors; induces eosinophil shape change with an EC50 of 3 nM. Also available as part of the Histamine H3 Receptor Tocriset™.

Licensing Information

Sold with the permission of SCI, Amsterdam

Technical Data

M. Wt 470.65
Formula C14H17ClN4S.2HBr
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 145231-35-2
PubChem ID 11213569
InChI Key JIJQPEZAVLJZBO-UHFFFAOYSA-N
Smiles Br.Br.ClC1=CC=C(CNC(=N)SCCCC2=CNC=N2)C=C1

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

SolubilitySoluble to 100 mM in water

Preparing Stock Solutions

The following data is based on the product molecular weight 470.65. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.12 mL 10.62 mL 21.25 mL
5 mM 0.42 mL 2.12 mL 4.25 mL
10 mM 0.21 mL 1.06 mL 2.12 mL
50 mM 0.04 mL 0.21 mL 0.42 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.

Buckland et al (2003) Histamine induces cytoskeletal changes in human eosinophils via the H4 receptor. Br.J.Pharmacol. 140 1117 PMID: 14530216

Liu et al (2001) Cloning and pharmacological characterization of a fourth histamine receptor (H4) expressed in bone marrow. Mol. Pharmacol. 59 420 PMID: 11179434

Yokoyama et al (1994) Clobenpropit (VUF-9153), a new histamine H3 receptor antagonist, inhibits electrically induced convulsions in mice. Eur.J.Pharmacol. 260 23 PMID: 7957622

Van der Goot et al (1992) Isothiourea analogues of histamine as potent agonists or antagonists of the histamine H3 receptor. Eur.J.Med.Chem. 27 511 PMID:


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View all Histamine H3 Receptor Antagonists

Keywords: Clobenpropit dihydrobromide, supplier, H4, partial, agonists, H3, antagonists, inverse, potent, Receptors, Histamine, histaminergic, VUF9153, VUF, 9153, Histamine, H3, Receptors, Histamine, H4, Receptors, Histamine, H3, Receptors, Tocris Bioscience

3 Citations for Clobenpropit dihydrobromide

Citations are publications that use Tocris products. Selected citations for Clobenpropit dihydrobromide include:

Femenia et al (2015) Hippocampal-Dependent Antidepressant Action of the H3 Receptor Antagonist Clobenpropit in a Rat Model of Depression. Int J Neuropsychopharmacol 18 PMID: 25762718

Alkan et al (2015) Histidine Decarboxylase Deficiency Prevents Autoimmune Diabetes in NOD Mice. J Immunol 2015 965056 PMID: 26090474

Hedegaard et al (2012) Molecular pharmacology of human NMDA receptors. Neurochem Int 61 601 PMID: 22197913


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