Biological Activity
High affinity and selective 5-HT7 antagonist (pKi = 8.14). Exhibits selectivity for 5-HT7 over other 5-HT receptors. Inhibits 5-HT-induced cAMP accumulation in HEK-293 cells expressing the 5-HT7 receptor. Orally bioavailable.
Compound Libraries
DR 4485 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 491.88 |
| Formula | C26H28Cl2N2O.HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 402942-53-4 |
| PubChem ID | 90488996 |
| InChI Key | QAERYGXKDZHTFR-UHFFFAOYSA-N |
| Smiles | ClC1=C2C(C3(CCCCN4CCC(C5=CC=C(Cl)C=C5)=CC4)CCC2)=C(NC3=O)C=C1.Cl |
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 | 49.19 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 491.88. 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 | 2.03 mL | 10.17 mL | 20.33 mL |
| 5 mM | 0.41 mL | 2.03 mL | 4.07 mL |
| 10 mM | 0.2 mL | 1.02 mL | 2.03 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.41 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Kikuchi et al (2003) New tetrahydrobenzindoles as potent and selective 5-HT(7) antagonists with increased In vitro metabolic stability. Bioorg.Med.Chem.Lett. 13 61 PMID: 12467617
Medina et al (2009) Synthesis of new serotonin 5-HT7 receptor ligands. Determinants of 5-HT7/5-HT1A receptor selectivity. J.Med.Chem. 52 2384 PMID: 19326916
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