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Tocris/Thioperamide/0644/50/50 mg

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货号: 0644/50

品牌: Tocris

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Description: H₃ antagonist and H₄ inverse agonist

Chemical Name: N-Cyclohexyl-4-(imidazol-4-yl)-1-piperidinecarbothioamide

Purity: ≥99% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Potent histamine H₃ and H₄ antagonist/inverse agonist. K_i 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.

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

Product Datasheets

Certificate of Analysis / Product Datasheet

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

Keywords: Thioperamide, supplier, H4, inverse, agonists, H3, antagonists, Receptors, Histamine, histaminergic, Histamine, H3, Receptors, Histamine, H4, Receptors, Histamine, H3, Receptors, Tocris Bioscience

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