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PB 28 dihydrochloride
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.
|Storage||Desiccate at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|water||8.87||20 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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.2 mM||11.27 mL||56.37 mL||112.74 mL|
|1 mM||2.25 mL||11.27 mL||22.55 mL|
|2 mM||1.13 mL||5.64 mL||11.27 mL|
|10 mM||0.23 mL||1.13 mL||2.25 mL|
References are publications that support the biological activity of the product.
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
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
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1 Citation for PB 28 dihydrochloride
Citations are publications that use Tocris products. Selected citations for PB 28 dihydrochloride include:
Rennekamp et al (2016) σ1 receptor ligands control a switch between passive and active threat responses. Nat Chem Biol 12 552 PMID: 27239788
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