TC 2559 difumarate
Cat. No. 2737
Chemical Name: 4-(5-ethoxy-3-pyridinyl)-N-methyl-(
Biological ActivitySubtype-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.
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.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
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.
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.
Bencherif et al (2000) TC-2559: a novel orally active ligand selective at neuronal acetylcholine receptors. Eur.J.Pharmacol. 409 45. PMID: 11099699.
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Citations are publications that use Tocris products. Selected citations for TC 2559 difumarate include:
Sun et al (2009) Rosiglitazone inhibits alpha4 nicotinic acetylcholine receptor expression in human lung carcinoma cells through peroxisome proliferator-activated receptor gamma-independent signals. Mol Cancer Ther 8 110. PMID: 19139119.
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Keywords: TC 2559 difumarate, supplier, Selective, partial, agonists, α4β2, alpha4beta2, receptors, Nicotinic, Receptors, Acetylcholine, nAChR, TC2559, difumarate, Tocris Bioscience, Nicotinic (α4β2) Receptor Agonist products
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Potent positive allosteric modulator of α4β2 nAChRs; also inhibitor of (α4)2(β2)3, muscle-type and Torpedo nAChRs
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