GT 2016

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Cat.No. 2419 - GT 2016 | C19H31N3O | CAS No. 152241-24-2
Description: Selective H3 antagonist
Chemical Name: 5-Cyclohexyl-1-[4-(1H-imidazol-5-yl)-1-piperidinyl]-1-pentanone
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

High affinity H3 receptor antagonist (Ki = 43.8 nM). Displays selectivity against H1 and H2 receptors (IC50 >10 μM). Increases the release of histamine in the cerebral cortex. Displays no activity at histamine methyltransferase in vitro at concentrations up to 3 μM. Brain penetrant.

Technical Data

M. Wt 317.47
Formula C19H31N3O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 152241-24-2
PubChem ID 9839975
InChI Key YTCGNPGLMAECND-UHFFFAOYSA-N
Smiles O=C(CCCCC3CCCCC3)N(CC2)CCC2C1=CN=CN1

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 31.75 100
ethanol 31.75 100

Preparing Stock Solutions

The following data is based on the product molecular weight 317.47. 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 3.15 mL 15.75 mL 31.5 mL
5 mM 0.63 mL 3.15 mL 6.3 mL
10 mM 0.31 mL 1.57 mL 3.15 mL
50 mM 0.06 mL 0.31 mL 0.63 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Tedford et al (1995) Pharmacological characterization of GT-2016, a non-thiourea-containing histamine H3 receptor antagonist: in vitro and in vivo studies. J.Pharmacol.Exp.Ther. 275 598 PMID: 7473144

Tedford et al (1999) Development of trans-2-[1H-imidazol-4-yl] cyclopropane derivatives as new high-affinity histamine H3 receptor ligands. J.Pharmacol.Exp.Ther. 289 1160 PMID: 10215700

Yates et al (1999) Identification and pharmacological characterization of a series of new 1H-4-substituted-imidazoyl histamine H3 receptor ligands. J.Pharmacol.Exp.Ther. 289 1151 PMID: 10215699


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Keywords: GT2016 histamine h3 antagonists histaminergic selective brain penetrant centrally active Histamine H3 Receptors

Citations for GT 2016

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