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.
| 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
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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