Biological Activity
High affinity σ2 receptor agonist (Ki values are 0.8 and 15.2 nM for σ2 and σ1 receptors respectively) that displays minimal affinity at other receptors. Inhibits electrically evoked twitch in guinea pig bladder and ileum (EC50 values are 2.62 and 3.96 μM respectively). Displays antiproliferative and cytotoxic effects in SK-N-SH neuroblastoma and C6 glioma cells.
Technical Data
| M. Wt | 443.5 |
| Formula | C24H38N2O.2HCl |
| Storage | Desiccate at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 172907-03-8 |
| PubChem ID | 46861545 |
| InChI Key | DSRBJOQIBXACIV-UHFFFAOYSA-N |
| Smiles | O=C1C=C(C)C(/C(C)=N/C2=C(N)C=CC=C2)=C(O)N1O.Cl.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 | |||
| water | 8.87 | 20mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 443.5. 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 | 2.25 mL | 11.27 mL | 22.55 mL |
| 5 mM | 0.45 mL | 2.25 mL | 4.51 mL |
| 10 mM | 0.23 mL | 1.13 mL | 2.25 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.45 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Berardi et al (1996) New σ and 5-HT1A receptor ligands: ω-(tetralin-1-yl)-n-alkylamine derivatives. J.Med.Chem. 39 176 PMID: 8568804
Colabufo et al (2003) A new method for evaluating σ2 ligand activity in the isolated guinea-pig bladder. Naunyn-Schmied.Arch.Pharmacol. 368 106 PMID:
Colabufo et al (2004) Antiproliferative and cytotoxic effects of some σ2 agonists and σ1 antagonists in tumour cell lines. Naunyn-Schmied.Arch.Pharmacol. 370 106 PMID:
Keywords: PB 28 dihydrochloride, supplier, High, affinity, σ2, sigma2, agonists, Receptors, PB28, dihydrochloride, Sigma2, Receptors, Sigma2, Receptors, Tocris Bioscience
