VUF 10166

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Cat.No. 4532 - VUF 10166 | C13H15ClN4 | CAS No. 155584-74-0
Description: High affinity 5-HT3 receptor antagonist
Chemical Name: 2-Chloro-3-(4-methyl-1-piperazinyl)quinoxaline
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

High affinity 5-HT3 receptor antagonist (IC50 values are 0.04 and 22 nM for human 5HT3A and 5-HT3AB receptors respectively). Exhibits partial agonist activity at 5-HT3A receptors at higher concentrations (EC50 = 5.2 μM). Also histamine H4 receptor antagonist (pKi = 6.64 in HEK cells).

Technical Data

M. Wt 262.74
Formula C13H15ClN4
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 155584-74-0
PubChem ID 24278976
InChI Key FFXVTQDGTKEXHF-UHFFFAOYSA-N
Smiles ClC2=NC1=CC=CC=C1N=C2N3CCN(C)CC3

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 26.27 100
ethanol 26.27 100

Preparing Stock Solutions

The following data is based on the product molecular weight 262.74. 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 3.81 mL 19.03 mL 38.06 mL
5 mM 0.76 mL 3.81 mL 7.61 mL
10 mM 0.38 mL 1.9 mL 3.81 mL
50 mM 0.08 mL 0.38 mL 0.76 mL

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Product Datasheets

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References

References are publications that support the products' biological activity.

Thompson et al (2012) VUF10166, a novel compound with differing activities at 5-HT3A and 5-HT3AB receptors. J.Pharmacol.Exp.Ther. 341 350 PMID: 22306960

Smits et al (2008) Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo. J.Med.Chem. 51 2457 PMID: 18357976


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View all 5-HT3 Receptor Antagonists

Keywords: 5-ht serotonin receptors antagonists high affinity partial agonists 5-ht3a 5-ht3ab 5-ht3 5ht VUF10166 5-HT3 Receptors

Citations for VUF 10166

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Literature in this Area

5-HT Receptors

5-HT Receptors Scientific Review

Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.

Pathways for VUF 10166

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