Thioperamide

Pricing Availability Delivery Time Qty
Cat.No. 0644 - Thioperamide | C15H24N4S | CAS No. 106243-16-7
Description: H3 antagonist and H4 inverse agonist
Chemical Name: N-Cyclohexyl-4-(imidazol-4-yl)-1-piperidinecarbothioamide
Purity: ≥99% (HPLC)
Datasheet
Citations (4)
Literature

Biological Activity

Potent histamine H3 and H4 antagonist/inverse agonist. Ki values are 25 and 27 nM for human recombinant H3 and H4 receptors respectively. Blocks eosinophil shape change (IC50 = 1.4 μM) and chemotaxis (IC50 = 519 nM) induced by histamine. Freely crosses the blood-brain barrier. Also available as part of the Histamine H3 Receptor Tocriset™.

Compound Libraries

Thioperamide is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 292.44
Formula C15H24N4S
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 106243-16-7
PubChem ID 3035905
InChI Key QKDDJDBFONZGBW-UHFFFAOYSA-N
Smiles S=C(NC3CCCCC3)N(CC2)CCC2C1=CNC=N1

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 29.24 100
ethanol 29.24 100

Preparing Stock Solutions

The following data is based on the product molecular weight 292.44. 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 3.42 mL 17.1 mL 34.2 mL
5 mM 0.68 mL 3.42 mL 6.84 mL
10 mM 0.34 mL 1.71 mL 3.42 mL
50 mM 0.07 mL 0.34 mL 0.68 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.

Gbahou et al (2006) Compared pharmacology of human H3 and H4 receptors: structure-activity relationships of histamine derivatives. Br.J.Pharmacol. 147 744 PMID: 16432504

Hew et al (1990) Characterisation of histamine H3 receptors in guinea pig ileum with H3 selective ligands. Br.J.Pharmacol. 101 621 PMID: 1963802

Ling et al (2004) Histamine H4 receptor mediates eosinophil chemotaxis with cell shape change and adhesion molecule upregulation. Br.J.Pharmacol. 142 161 PMID: 15131002

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


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View Related Products by Product Action

View all Histamine H3 Receptor Antagonists

Keywords: H4 inverse agonists H3 antagonists Receptors Histamine histaminergic Histamine H3 Receptors

4 Citations for Thioperamide

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

Francis et al (2012) Inhibition of histidine decarboxylase ablates the autocrine tumorigenic effects of histamine in human cholangiocarcinoma. Gut 61 753 PMID: 21873469

Holden et al (2007) Potentiation of NF-κB-dependent transcription and inflammatory mediator release by histamine in human airway epithelial cells. Saudi J Biol Sci 152 891 PMID: 17891168

Takahashi et al (2002) Targeted disruption of H3 receptors results in changes in brain histamine tone leading to an obese phenotype. J Clin Invest 110 1791 PMID: 12488429

Robinson and Dickenson (2001) Activation of the p38 and p42/p44 mitogen-activated protein kinase families by the histamine H(1) receptor in DDT(1)MF-2 cells. Br J Pharmacol 133 1378 PMID: 11498525


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