Bioactivity | LY393615 (NCC1048) is a novel neuronal Ca2+ (calcium channel) and Na + channel (sodium channel) blocker with IC50s of 1.9 μΜ and 5.2 μΜ for α1A and α1B calcium channel subunits. LY393615 has good brain penetration and neuroprotective effects in models of in cerebral ischemia that can be used for neurological disease research[1]. |
Invitro | LY393615 (0-10 μM) 抑制 HEK293 细胞的钙通量,对 α1A 和 α1B 钙通道亚基的 IC50 分别为 1.9 μM 和 5.2 μM,抑制分离的 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) 保护大脑免受低氧低血糖损伤,并对沙鼠全脑缺血引起的海马损伤提供显着保护[1]。LY393615 (腹腔注射 15 mg/kg;静脉注射 1 mg/kg) 有具有良好的脑渗透性,T1/2 分别为 2.04 小时 (静脉注射) 和 2.5 小时 (静脉注射) [1]。 Animal Model: |
Name | LY393615 |
CAS | 325819-97-4 |
Formula | C21H26ClF2NO |
Molar Mass | 381.89 |
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]. O'Neill MJ, et.al. LY393615, a novel neuronal Ca(2+) and Na(+) channel blocker with neuroprotective effects in models of in vitro and in vivo cerebral ischemia. Brain Res. 2001 Jan 5;888(1):138-149. |