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编 号：F757463
分子式：C21H26ClF2NO
分子量：381.89
分子式：C21H26ClF2NO
分子量：381.89
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CAS No: 325819-97-4
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生物活性：
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.
体内研究：
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。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) 。 Pharmacokinetic parameters for LY393615 in GerbilsRouteDose (mg/kg)T1/2 (h)
i.v.12.04
i.p.152.5
Animal Model:Gerbils global cerebral ischaemia
Dosage:10, 12.5 or 15 mg/kg
Administration:Intraperitoneal injection (i.p.)
Result:Protected against hypoxiahypoglycaemic insults in brain slices and also provided significant protection against ischaemia-induced hippocampal damage in gerbil global cerebral ischaemia.
Animal Model:Gerbils (Pharmacokinetic assay)
Dosage:1.0 or 15 mg/kg
Administration:Intraperitoneal injection (i.p.) ; Intravenous injection (i.v.)
Result:Had good brain penetration with T1/2s of 2.04 hours (i.v.) and2.5 hours (i.p.).
体外研究：
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。
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.
体内研究：
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。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) 。 Pharmacokinetic parameters for LY393615 in GerbilsRouteDose (mg/kg)T1/2 (h)
i.v.12.04
i.p.152.5
Animal Model:Gerbils global cerebral ischaemia
Dosage:10, 12.5 or 15 mg/kg
Administration:Intraperitoneal injection (i.p.)
Result:Protected against hypoxiahypoglycaemic insults in brain slices and also provided significant protection against ischaemia-induced hippocampal damage in gerbil global cerebral ischaemia.
Animal Model:Gerbils (Pharmacokinetic assay)
Dosage:1.0 or 15 mg/kg
Administration:Intraperitoneal injection (i.p.) ; Intravenous injection (i.v.)
Result:Had good brain penetration with T1/2s of 2.04 hours (i.v.) and2.5 hours (i.p.).
体外研究：
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。
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