Clobenpropit dihydrobromide

Name: Clobenpropit dihydrobromide
Brand: Tocris Bioscience
SKU: 0752

Catalog # 0752

Citations (4)

COA / SDS

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Key Product Details

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)
Molecular Weight:	470.65

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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.

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	water		100

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 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	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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References

References are publications that support the biological activity of the product.

Buckland Histamine induces cytoskeletal changes in human eosinophils via the H₄ receptor. Br.J.Pharmacol. 2003 PMID: 14530216
Liu Cloning and pharmacological characterization of a fourth histamine receptor (H₄) expressed in bone marrow. Mol. Pharmacol. 2001 PMID: 11179434
Yokoyama Clobenpropit (VUF-9153), a new histamine H₃ receptor antagonist, inhibits electrically induced convulsions in mice. Eur.J.Pharmacol. 1994 PMID: 7957622
Van der Goot Isothiourea analogues of histamine as potent agonists or antagonists of the histamine H₃ receptor. Eur.J.Med.Chem.

Citations for Clobenpropit dihydrobromide (4)

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Citations are publications that use Bio-Techne products. Selected citations for Clobenpropit dihydrobromide include:

Alkan et al. (2015) Histidine Decarboxylase Deficiency Prevents Autoimmune Diabetes in NOD Mice. J Immunol. 2015:965056
PMID: 26090474
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
Hedegaard et al. (2012) Molecular pharmacology of human NMDA receptors. Neurochem Int. 61:601
PMID: 22197913
Flamand et al. (2004) Histamine-induced inhibition of leukotriene biosynthesis in human neutrophils: involvement of the H2 receptor and cAMP. Br J Pharmacol. 141:552
PMID: 14744809

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