沙芬酰胺 T6651L

Product Introduction
Bioactivity


英文名: Safinamide

描述: Safinamide (FCE-26743) 是一种可逆选择性单胺氧化酶 B (IC50 0.098μM)抑制剂，可减少多巴胺的降解，也是一种谷氨酸释放抑制剂(IC50 8μM)。它还能抑制多巴胺的再摄取。 Safinamide 还能阻断钠和钙通道。 Safinamide 的潜在的其他用途可能是帕金森病、不宁腿综合征和癫痫。

体外活性: Safinamide（1-300 µM）以浓度依赖的方式减少峰值钠电流的幅度。当保持电位去极化至-53 mV时，safinamide在大鼠皮质神经元中展现出较低的IC50值（8 µM）的抑制效果[1]。

体内活性: Daily intraperitoneal injections of Safinamide 1mg/kg were administered for 14 days and the treatment prior to MCAO significantly ameliorates MCAO-caused cerebral infarction volume, neurological deficit, disruption of the brain-blood barrier (BBB), and impairs expression of tight junction protein occludin and ZO-1 in mice .Safinamide (intraperitoneal injection; 5 mg/kg, 15 mg/kg and 30 mg/kg) dose dependently inhibits the veratridine-induced GABA release and Glu release in vivo [2].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (165.38 mM)


关键字: Safinamide

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相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Approved Drug Library | FDA-Approved & Pharmacopeia Drug Library | Mitochondria-Targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | Inhibitor Library | EMA Approved Drug Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途