| Description | CVN417 is an orally active antagonist of nAChR containing the α6 subunit, modulating phasic dopaminergic neurotransmission in an impulse-dependent fashion. It inhibits Ca(2+) efflux through nAChR subunits, displaying IC50 values of 0.086 μM (α6), 2.56 μM (α3), and 0.657 μM (α4). CVN417 has shown efficacy in reducing resting tremor in rodent models, suggesting a potential to ameliorate movement disorders in conditions like Parkinson's disease [1]. |
| In vitro | CVN417(10 μM; 0-2 h)在人类肝微粒和肝细胞展示了较低的代谢周转率[1]。体外ADME数据显示,CVN417在不同物种肝微粒的Cl int(μL/min/mg)值分别为:人2.8,大鼠31.2,小鼠33.3,犬27.7;在肝细胞中的比值(mL/min/10^6 cells)为:人3.7,大鼠20.8,小鼠25.1,犬32.3[1]。 |
| molecular weight | N/A |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |