| Bioactivity | CVN417 is an orally active α6 subunit-containing nAChR antagonist, modulating phasic dopaminergic neurotransmission in an impulse-dependent manner. CVN417 inhibits Ca(2+) effluents mediated by nAChR subunits with IC50s of 0.086 μM (α6), 2.56 μM (α3) and 0.657 μM (α4), respectively. CVN417 attenuates resting tremor in Rodent models, displays the potential to improve movement dysfunction, in conditions such as Parkinson's disease[1]. |
| Target | IC50: 0.086 μM (nAChR α6), 2.56 μM (nAChR α3), 0.657 μM (nAChR α4) |
| Invitro | CVN417 (10 μM; 0-2 h) 在人肝微粒或肝细胞中表现出较低的代谢周转特性[1]。CVN417 的体外 ADME 数据[1] |
| In Vivo | CVN417 (3 mg/kg, 10 mg/kg, 25 mg/kg; 口服) 大鼠震颤模型中震颤下颌运动持续时间呈剂量依赖性减少[1]。在大鼠中对 CVN417 的药代动力学分析[1]Route |
| Name | CVN417 |
| CAS | 2919851-73-1 |
| Formula | C18H23ClN4O2 |
| Molar Mass | 362.85 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Christie LA, et al. Discovery of CVN417, a Novel Brain-Penetrant α6-Containing Nicotinic Receptor Antagonist for the Modulation of Motor Dysfunction. J Med Chem. 2023 Aug 31. |