Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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].
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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) exhibits a lower metabolic turnover in human liver microsomes or hepatocytes [1]. In vitro ADME data for CVN417 [1] across various species demonstrate the following intrinsic clearance rates: human liver microsomes Cl int (μL/min/mg) 2.8, rat 31.2, mouse 33.3, dog 27.7; and in hepatocytes (mL/min/10^6 cells) human 3.7, rat 20.8, mouse 25.1, dog 32.3. |
Molecular Weight | N/A |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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