HEC30654

**HEC30654** is a selective small molecule antagonist of the serotonin 5-HT6 receptor (IC50 = 1.1 nM for affinity, 15 nM for antagonism), exhibiting higher potency than comparators like LuAE58054. Developed for symptomatic treatment of cognitive disorders, particularly Alzheimer's disease, it demonstrated procognitive effects in preclinical rodent models of scopolamine-induced dysfunction and has a long half-life (52-64 hours in humans). In a Phase I single ascending dose trial (5-60 mg oral) in healthy Chinese subjects, doses up to 30 mg were safe and well-tolerated with supraproportional pharmacokinetics, primarily fecal elimination unchanged, and minimal metabolism to weak antagonist HEC93263; higher doses triggered safety stopping rules due to immune-related adverse events.[1][6]

Other names

HEC30654AcOHHEC-30654AcOHHEC 30654AcOH