| Description | ML218 is an orally active, selective, potent, and blood-brain barrier-crossing inhibitor of T-type Ca2+ channels (Cav3.1, Cav3.2, Cav3.3) (IC50 for Cav3.2 and Cav3.3 is 310 nM and 270 nM, respectively).ML218 inhibits the burst activity of neurons in the subthalamic nucleus (STN). |
| In vitro | 在电压钳实验中，对 ML218 进行 3μM 的浴液应用显著降低了约 45% 的 T 型钙离子电流[1]。 |
| In vivo | 在通过氟哌啶醇诱导的 Sprague-Dawley 雄性大鼠（275-299 g）中，ML218（0.03 mg/kg，0.1 mg/kg，0.3 mg/kg，1 mg/kg，3mg/kg，10 mg/kg，30mg/kg；口服给药；一次）处理能够逆转由 0.75 mg/kg 氟哌啶醇诱导的大鼠僵直行为[1]。 |
| Target activity | Cav3.3:270 nM, 270 nM:Ca2+ flux, Cav 3.2:310 nM |
| molecular weight | 369.33 |
| Molecular formula | C19H26Cl2N2O |
| CAS | 1346233-68-8 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 100 mg/mL (270.76 mM), Sonication is recommended. |
| References | 1. Xiang Z, et al. The Discovery and Characterization of ML218: A Novel, Centrally Active T-Type Calcium Channel Inhibitor with Robust Effects in STN Neurons and in a Rodent Model of Parkinson's Disease. ACS Chem Neurosci. 2011 Dec 21;2(12):730-742. |