TC-2559 (difumarate)

TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM) . TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 μM. Antinociceptive effect[1][2].

Product Specifications

CAS Number

[2454492-41-0]

UNSPSC

12352005

Target

NAChR

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/tc-2559-difumarate.html

Purity

98.4

Solubility

H2O : 43.84 mg/mL (ultrasonic; warming)

Smiles

CCOC1=CN=CC(/C=C/CCNC)=C1.O=C(/C=C/C(O)=O)O.O=C(/C=C/C(O)=O)O

Molecular Formula

C20H26N2O9

Molecular Weight

438.43

References & Citations

[1]Bencherif M, et al. TC-2559: a novel orally active ligand selective at neuronal acetylcholine receptors. Eur J Pharmacol. 2000;409 (1) :45-55.|[2]Cheng LZ, et al. Enhanced inhibitory synaptic transmission in the spinal dorsal horn mediates antinociceptive effects of TC-2559. Mol Pain. 2011;7:56. Published 2011 Aug 4.