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Submit ReviewClobenpropit dihydrobromide
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)
Biological Activity for Clobenpropit dihydrobromide
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 for Clobenpropit dihydrobromide
| 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 Data for Clobenpropit dihydrobromide
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 100 |
Preparing Stock Solutions for Clobenpropit dihydrobromide
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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Product Datasheets for Clobenpropit dihydrobromide
References for Clobenpropit dihydrobromide
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for Clobenpropit dihydrobromide, please let us know.
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Keywords: Clobenpropit dihydrobromide, Clobenpropit dihydrobromide supplier, H4, partial, agonists, H3, antagonists, inverse, potent, Receptors, Histamine, histaminergic, VUF9153, VUF, 9153, 0752, Tocris Bioscience
4 Citations for Clobenpropit dihydrobromide
Citations are publications that use Tocris 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
Hedegaard et al (2012) Molecular pharmacology of human NMDA receptors. Neurochem Int 61 601 PMID: 22197913
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
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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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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Written by Iwan de Esch and Rob Leurs, this review provides a synopsis of the different histamine receptor subtypes and the ligands that act upon them; compounds available from Tocris are listed.
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