Biological Activity
Subtype-selective partial agonist for α4β2 nicotinic acetylcholine receptors (EC50 values are 0.18, 12.5, 14.0, > 30, > 100 and > 100 μM for α4β2, α4β4, α2β4, α3β4, α3β2 and α7 receptor subtypes respectively). Displays selectivity for (α4)2(β2)3 receptor stoichiometry and enhanced CNS-PNS selectivity ratio. Attenuates scopolamine-induced cognitive deficits in a step-through passive avoidance task.
Technical Data
| M. Wt | 438.43 |
| Formula | C12H18N2O.2C4H4O4 |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 212332-35-9 |
| PubChem ID | 56972184 |
| InChI Key | GEWVPSJQGJBDLM-MYBAKCFCSA-N |
| Smiles | CCOC1=CN=CC(/C=C/CCNC)=C1.O=C(O)/C=C/C(O)=O.O=C(O)/C=C/C(O)=O |
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 | 43.84 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 438.43. 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 | 2.28 mL | 11.4 mL | 22.81 mL |
| 5 mM | 0.46 mL | 2.28 mL | 4.56 mL |
| 10 mM | 0.23 mL | 1.14 mL | 2.28 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Bencherif et al (2000) TC-2559: a novel orally active ligand selective at neuronal acetylcholine receptors. Eur.J.Pharmacol. 409 45 PMID: 11099699
Chen et al (2003) The nicotinic α4β2 receptor selective agonist, TC-2559, increases dopamine neuronal activity in the ventral tegmental area of rat midbrain slices. Neuropharmacology 45 334 PMID: 12871651
Zwart et al (2006) 5-I A-85380 and TC-2559 differentially activate heterologously expressed α4β2 nicotinic receptors. Eur.J.Pharmacol. 539 10 PMID: 16674940
Keywords: TC 2559 difumarate, supplier, Selective, partial, agonists, α4β2, alpha4beta2, receptors, Nicotinic, Receptors, Acetylcholine, nAChR, TC2559, difumarate, Nicotinic, (a4b2), Receptors, Nicotinic, (a4b2), Receptors, Tocris Bioscience
