| Description | LY393615 (NCC1048) is a novel blocker of both neuronal Ca²⁺ (calcium) and Na⁺ (sodium) channels, exhibiting half-maximal inhibitory concentrations (IC₅₀) of 1.9 µM and 5.2 µM against α1A and α1B calcium channel subunits, respectively. This compound demonstrates effective brain penetration and has shown neuroprotective effects in cerebral ischemia models, suggesting its utility in neurological disease research [1]. |
| In vitro | LY393615（0-10 μM）在抑制HEK293细胞的钙通量方面表现出效力，对α1A及α1B钙通道亚基的半抑制浓度(IC50)分别为1.9 μM与5.2 μM，同时该化合物对孤立的Purkinje细胞中的P型钙通道的IC50为4.0 μM[1]。 |
| In vivo | LY393615（12.5或15 mg/kg，腹腔注射，单次）能有效地保护大脑免遭低氧低血糖引起的损伤，并显著抵御全脑缺血导致的沙鼠海马区损伤。此外，不同给药方式下该化合物在脑部的药动学参数显示，其具有良好的脑渗透性，半衰期（T 1/2）分别为2.04小时（静脉注射1 mg/kg）和2.5小时（腹腔注射15 mg/kg）。【1】 |
| Target activity | Ca2+ channel, P/Q-type:4 μM |
| Synonyms | NCC1048 |
| molecular weight | N/A |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |