tc 25

partial agonist of α4β2 nicotinic acetylcholine receptor

TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist with an EC 50 of 0.18 μM. It exhibits selectivity for α4β2 receptors over α2β4, α4β4, and α3β4 receptors, with EC 50 s ranging from 10 to 30 μM. TC-2559 difumarate also demonstrates antinociceptive effects.

PTC258为针对伸长复合体蛋白1基因（ELP1）的特异性口服基因剪接调节剂，能促进ELP1在体外和体内的表达增加，并在小鼠模型中显示出良好的耐受性。