Biological Activity
High affinity and subtype selective α6β2 and α4β2 partial agonist (Ki values are 12 and 26nM for rat α6β2 and α4β2 receptors respectively). Has low affinity for α3β4 and α7 receptors (Ki values are 4.8 and 13 μM for human α3β4 and rat α7 receptors respectively). Stimulates dopamine release from striatal slices in vitro. Attenuates nicotine-induced self-administration and conditional place preference in rats.
Compound Libraries
CC4 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 406.52 |
| Formula | C24H30N4O2 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 492-02-4 |
| PubChem ID | 91654624 |
| InChI Key | LEXDAVFCJPDCNA-VNTMZGSJSA-N |
| Smiles | O=C1N2C([C@@](C3)([H])CN(CCN5C[C@](C6)([H])C(N4C[C@]6([H])C5)=CC=CC4=O)C[C@@]3([H])C2)=CC=C1 |
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 | 40.65 | 100 | |
| water | 8.13 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 406.52. 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 | 2.46 mL | 12.3 mL | 24.6 mL |
| 5 mM | 0.49 mL | 2.46 mL | 4.92 mL |
| 10 mM | 0.25 mL | 1.23 mL | 2.46 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.49 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Sala et al (2013) CC4, a dimer of cytisine, is a selective partial agonist at α4β2/α6β2 nAChR with improved selectivity for tobacco smoking c Br.J.Pharmacol. 168 835 PMID: 22957729
Riganti et al (2005) Long-term exposure to the new nicotinic antagonist 1,2-bisN-cytisinylethane upregulates nicotinic receptor subtypes of SH-SY5Y human neuroblastoma cells. Br.J.Pharmacol. 146 1096 PMID: 16273122
Carbonnelle et al (2003) Nitrogen substitution modifies the activity of cytisine on neuronal nicotinic receptor subtypes. Eur.J.Pharmacol. 471 85 PMID: 12818695
Keywords: CC4, supplier, CC4, high, affinity, subtype, selective, partial, agonist, acetylcholine, nicotinic, receptors, alpha4beta2, a4b2, α4β2, alpha6beta3, a6b3, α6β3, Nicotinic, (a4b2), Receptors, Nicotinic, Receptors, (Other, Subtypes), Nicotinic, (a4b2), Receptors, Tocris Bioscience
